RU2651892C2 - Nucleoside phosphoramidates as antiviral agents - Google Patents

Abstract

FIELD: chemistry.

SUBSTANCE: present invention relates to isopropyl ester of (S)-2-{[(2R, 3R, 4R, 5R)-5-(2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl)-4-fluoro-3-hydroxy-4-methyl-tetrahydrofuran-2-ylmethoxy]-phenoxy-phosphorylamino}-propionic acid and its stereoisomer, which can be used to treat viral infections in mammals, a method for its preparation, compositions based thereon and its use in treatment of viral diseases. Proposed method comprises reaction of compounds

and

where X′ is a leaving group.

EFFECT: disclosed is a novel effective agent for treating diseases, caused by hepatitis A and C viruses, West Nile fever, yellow fever, dengue fever, diarrhea of cattle, Japanese encephalitis, rhinovirus, poliovirus, and an effective method for production thereof.

7 cl, 82 ex, 32 tbl

Description

Technical field

The present invention relates to nucleoside phosphoramidates and their use as agents for the treatment of viral diseases. These compounds are inhibitors of RNA-dependent replication of viral RNA, and they are also effective as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication, as well as for the treatment of hepatitis C, in mammals. The invention provides new chemical compounds and methods of using these compounds individually or in combination with other antiviral agents for the treatment of hepatitis C.

State of the art

Hepatitis C virus (HCV) infection is a major health problem leading to chronic liver diseases, such as cirrhosis and hepatocellular carcinoma, in a significant number of infected individuals, representing about 2-15% of the global population. According to a study by U.S. Center for Disease Control, there are 2.5 million people infected in the United States alone. According to the World Health Organization, there are more than 200 million people infected worldwide, and 3 to 4 million are infected every year. Only 20% of those infected are cured, and the rest can be carriers of HCV for the rest of their lives. Ten to twenty percent of chronically infected individuals develop liver-damaging cirrhosis or cancer over time. A viral disease is transmitted parenterally through infected blood and blood products, infected needles, or sexually and vertically from infected mothers or transferring mothers to the fetus. Conventional methods for treating HCV infection, limited to immunotherapy using recombinant interferon-α alone, or in combination with the nucleoside analog ribavirin, have limited clinical results. Moreover, there is no recognized HCV vaccine. To summarize, there is an urgent need for improved therapeutic agents to combat chronic hepatitis C virus infection.

Virion HCV is a positively helical enveloped RNA-containing virus with one oligoribonucleotide genomic sequence consisting of approximately 9600 bases encoding a polyprotein consisting of approximately 3.010 nitrogen bases. Protein products of the HCV gene include structural proteins C, E1 and E2, and non-structural proteins NS2, NS3, NS4A and NS4B, and NS5A and NS5B. Non-structural (NS) proteins are thought to provide a catalytic mechanism for viral replication. The NS3 protease releases NS5B, an RNA-dependent polymerase, from the polyprotein chain. HCV NS5B polymerase is required for the synthesis of double-stranded RNA with single-stranded viral RNA serving as a template in the HCV replication cycle. Therefore, NS5B polymerase is recognized as the main component of the HCV replicative complex (K. Ishi, et al, Heptology, 1999, 29: 1227-1235; V. Lohmann, et al., Virology, 1998, 249: 108-118). Inhibition of HCV NS5B polymerase inhibits the formation of double-stranded HCV RNA, and therefore represents a promising approach to the development of HCV-specific antiviral therapy.

HCV belongs to a large family of viruses that have common features.

Flaviviridae viruses

The Flaviviridae virus family includes at least three distinct genera: pestiviruses, which cause diseases in cattle and pigs; flaviviruses, the main cause of such diseases, dengue fever and yellow fever; and hepaciviruses, of which HCV is the only member. The genus flaviviruses includes more than 68 members, divided into groups according to the principle of serological similarity (Calisher et al., J. Gen. Virol, 1993, 70, 37-43). The clinical manifestations of diseases vary and include fever, encephalitis, and hemorrhagic fever (Fields Virology, Editors: Fields, B.N., Knipe, DM, and Howley, PM, Lippincott-Raven Publishers, Philadelphia, PA, 1996, Chapter 31, 931- 959). Flaviviruses of general interest are associated with human diseases such as Dengue hemorrhagic fever (DHF), yellow fever virus, shock syndrome and Japanese encephalitis virus (Halstead, S. B., Rev. Infect. Dis., 1984, 6, 251 -264; Halstead, S.V., Science, 239: 476-481, 1988; Monath, TP, New Eng. J. Med, 1988, 319, 64 1-643).

The pestivirus genus includes bovine viral diarrhea virus (BVDV), classical swine fever virus (CSFV, also called swine cholera virus), and sheep border disease virus (BDV) (Moennig, V. et al. Adv. Vir. Res. 1992, 41, 53-98). Infections of livestock (cattle, sheep, pigs) caused by pestiviruses are causing serious economic losses around the world. BVDV causes viral diarrhea in cattle and is of great economic importance for livestock production (Meyers, G. and livestock industry Thiel, HJ, Advances in Vims Research, 1996, 47, 53-118; Moennig V., et al, Adv. Vir Res. 1992, 41, 53-98). Human pestiviruses are not described to the same extent as animal pestiviruses. However, serological reviews indicate a significant effect of pestiviruses on the human body.

Pestiviruses and hepaciviruses are closely related groups within the Flaviviridae family. Other closely related species of this family include GB virus A, GB virus A-like agents, GB virus B and GB virus C (also called hepatitis G virus, HGV). The group of hepatitis viruses (hepatitis C virus, HCV) consists of several closely related, but genetically distinguishable viruses that infect humans. There are at least 6 HCV genotypes and more than 50 subtypes. Due to the similarity between pestiviruses and hepatitis viruses, combined with the poor ability of hepatitis viruses to grow in sufficient quantities in cell culture, it is often replaced by bovine viral diarrhea virus (BVDV) to study the HCV virus.

The genetic organization of pestiviruses and hepativiruses is very similar. These positively helical RNA viruses have one large open reading frame (ORF) encoding all the viral proteins necessary for virus replication. These proteins are expressed as polyproteins, which are co- and post-translationally processed by both cellular and virus-encoded proteinases to assemble mature viral proteins. The viral proteins responsible for the replication of the viral RNA genome are located approximately at the carboxy-terminal site. Two-thirds of ORFs encode non-structural (NS) proteins. The genetic organization and processing of polyproteins for the ORF region encoding non-structural proteins, pestiviruses and hepatitis viruses is very similar. For both pestiviruses and hepaciviruses, mature non-structural (NS) proteins, in a predetermined sequence from the amino-terminal portion of the non-structural protein coding region to the carboxy-terminal ORF region, consist of p7, NS2, NS3, NS4A, NS4B, NS5A, and NS5B.

NS proteins of both pestiviruses and hepativiruses contain the same sequence of domains that determine the specific functions of proteins. For example, the NS3 viral proteins in both groups contain fragments of amino acid sequences characterizing serine proteases and helicases (Gorbalenya et al., Nature, 1988, 333, 22; Bazan and Fletterick Virology, 1989,171,637-639; Gorbalenya et al., Nucleic Acid Res., 1989, 17, 3889-3897). Similarly, the NS4B proteins of pestiviruses and hepativiruses include fragments characterizing RNA-dependent RNA polymerases (Koonin, E.V. and Dolja, V.V., Crir. Rev. Biochem. Molec. Biol. 1993, 28, 375-430).

The actual role and functions of NS proteins of pestiviruses and hepativiruses in the life cycle of viruses are absolutely similar. In both cases, NS3 serine proteinase is responsible for all proteolytic processing of polyprotein precursors upstream from its initial position at ORF (Wiskerchen and Collett, Virology, 1991, 184, 341-350; Bartenschlager et al., J. Virol. 1993, 67 , 3835-3844; Eckart et al. Biochem. Biophys. Res. Comm. 1993,192, 399-406; Grakoui et al., J. Virol. 1993, 67, 2832-2843; Grakoui et al., Proc. Natl Acad Sci. USA 1993, 90, 10583-10587; Hijikata et al., J. Virol. 1993, 67, 4665-4675; Tome et al, J. Virol., 1993, 67, 4017-4026). The NS4A protein in both cases acts as a cofactor of the NS3 serine protease (Bartenschlager et al., J. Virol. 1994, 68, 5045-5055; Failla et al., J. Virol. 1994, 68, 3753-3760; Xu et al. , J. Virol., 1997, 71:53 12-5322). The NS3 protein of both virus groups also functions as helicase (Kim et al., Biochem. Biophys. Res. Comm., 1995, 215, 160-166; Jin and Peterson, Arch. Biochem Biophys., 1995, 323, 47-53; Warrener and Collett, J. Virol. 1995, 69, 1720-1726). Finally, NS5B proteins of both pestiviruses and hepatoviruses have predicted RNA-dependent RNA polymerase activity (Behrens et al., EMBO, 1996, 15, 12-22; Lechmann et al., J. Virol., 1997, 71, 8416 -8428; Yuan et al., Biochem Biophys. Res. Comm. 1997, 232, 231-235; Hagedorn, PCT WO 97/12033; Zhong et al, J. Virol., 1998, 72, 9365-9369).

Currently, treatment options for people infected with hepatitis C virus are limited. A currently accepted possibility is the use of immunotherapy using recombinant interferon-α alone, or in combination with the nucleoside analogue ribavirin. The clinical effectiveness of this therapy is limited, and only 50% of patients undergoing treatment have a response to therapy. Thus, there is a need to create new, more effective ways to treat HCV infection to solve this problem.

Currently, several potential molecular targets for drug development have been discovered, including, but not limited to, NS2-NS3 autoprotease, protease N ₃ , helicase N ₃ and polymerase NS5B. The replication of a single-stranded, positively directed RNA genome is impossible without an RNA-dependent RNA polymerase, and this enzyme is of particular interest among physicians.

HCV virus NS5B replication inhibitors: Tan, S.-L., et al., Nature Rev. were considered as possible methods of treating hepatitis C. Drug Discov., 2002, 1, 867-881; Walker, M.P. et al., Exp. Opin. Investigational Drugs, 2003, 12, 1269-1280; Ni, Z-J., Et al., Current Opinion in Drug Discovery and Development, 2004, 7, 446-459; Beaulieu, P. L., et al., Current Opinion in Investigational Drugs, 2004, 5, 838-850; Wu, J., et al., Current Drug Targets-Infectious Disorders, 2003, 3, 207-219; Griffith, R. C., et al, Annual Reports in Medicinal Chemistry, 2004, 39, 223-237; Carrol, S., et al., Infectious Disorders-Drug Targets, 2006, 6, 17-29. Attempts to detect new and more effective nucleosides that act as NS5B inhibitors of the hepatitis C virus continue because of the possibility of the emergence of resistant strains of the hepatitis C virus and the need to determine substances with a wide effect on the genotype.

Nucleoside NS5B polymerase inhibitors can act as an artificial substrate leading to chain termination, or as a competitive inhibitor that competes with the nucleotide that binds to the polymerase. In order to perform the function of a chain terminator, the nucleoside analogue must be removed from the cell and converted in vivo to triphosphate in order to compete for the nucleotide binding site. This conversion to triphosphate is usually mediated by cell kinases, which creates additional requirements for the structure of a potential nucleoside polymerase inhibitor. Unfortunately, this limits the accuracy of the assessment of nucleosides as inhibitors of HCV replication in cell assays that allow in situ phosphorylation.

In some cases, the biological activity of a nucleoside is hindered by its low substrate characteristics in relation to one or more kinases necessary for the transition to the active triphosphate form. The formation of monophosphate by a nucleoside kinase is generally considered to be a stage that limits the reaction rate of three phosphorylation. In order to circumvent the need for a phosphorylation initiation step in the metabolism of a nucleoside to an active triphosphate analogue, the preparation of stable phosphate prodrugs has been described. Nucleoside phosphoramidate prodrugs have been shown to be precursors of active nucleoside triphosphate, and inhibit viral replication when introduced into whole virus infected cells (McGuigan, C, et al., J. Med. Chem., 1996, 39, 1748-1753; Valette, G., et al., J. Med. Chem., 1996, 39, 1981-1990; Balzarini, J., et al., Proc. National Acad Sci USA, 1996, 93, 7295-7299; Siddiqui, AQ, et al., J. Med. Chem., 1999, 42,4122-4128; Eisenberg, EJ, et al., Nucleosides, Nucleotides and Nucleic Acids, 2001, 20, 1091-1098; Lee, WA, et al., Antimicrobial Agents and Chemotherapy, 2005, 49, 1898); US2006 / 0241064; and WO 2007/095269.

Also, the value of nucleotides as effective drugs is limited by their sometimes weak physicochemical and pharmacokinetic properties. These weak properties may limit intestinal absorption of the agent and absorption by the target tissue or cell. Nucleoside prodrugs were used to improve their properties. It was shown that the creation of nucleoside phosphoramidates improves the systemic absorption of the nucleoside and, in addition, the phosphoramidate part of these “pronucleotides” is closed by neutral lipophilic groups to achieve a suitable distribution coefficient for optimizing absorption and transport inside the cell, significantly increasing the intracellular concentration of the monosphosphate analog nucleoside relative to a single administration starting nucleoside. The result of enzyme-mediated hydrolysis of the ester portion of the phosphate is nucleoside monophosphate, and reaction-limiting phosphorylation is optional.

SUMMARY OF THE INVENTION

The present invention provides novel nucleoside derivative phosphoramidate prodrugs suitable for the treatment of viral infections in mammals, comprising compounds, stereoisomers, salts (acid or base addition salts), hydrates, solvates or crystalline forms of these compounds having the following structure:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl or naphthyl, where phenyl or naphthyl may contain at least one of a number of substituents: C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1- 6a} alkoxy, F, Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N ( R ^{1 ″} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^{1 "} represents -OR' or -N (R ^{1 '} ) ₂ ;

(b) R ² represents hydrogen, C _1-10 alkyl, R ^3a or R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms, C (O) CR ^3a R ^3b NHR ¹ , where n is from 2 to 4 and R ¹ , R ^3a , and R ^3b ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) _c (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ^{3 ″} , aryl and aryl C _1-3 alkyl, said aryl groups may contain a substituent selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen and R ^3b and R ² together represent (CH ₂ ) _n , so that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together they represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring N and C atoms, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3, f is from 2 to 5 , n is from 2 to 4, and where R ^{3 ′} is independently hydrogen or C _1-6 alkyl and R ^{3 ″} is —OR ^′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl and R ^3b represents H, where R ^{3 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _-1-10 alkyl, or C _{1 -6} alkyl, R ^{3 ″} or —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, optionally having a substituent from the series: lower alkyl, alkoxy, di (lower alkyl) amino, or hydrogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl such as phenyl, heteroaryl such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxyl lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, O, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X is H, OH, F, OMe, halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OC (O) O (C _1-4 alkyl), OC (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-10 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{2- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , N (C _1-18 acyl) ₂ , where alkyl, alkynyl alkenyl and vinyl are possible o, contain as substituent N ₃ , CN, from one to three halogens (Cl, Br, F, I), NO ₂ , C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _1-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , N (C _1-4 acyl) ₂ ;

the base, by its nature, belongs to modified purine or pyrimidine bases, represented by the following structures:

Where

Z represents N or CR ¹² ;

R ⁷ , R ⁸ , R ⁹ , R ¹⁰ , and R ¹¹ independently represent H, F, Cl, Br, I, OH, OR ', SH, SR' NH ₂ , NHR ', NR' ₂ , lower alkyl C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower C ₂ -C ₆ alkynyl, such as C≡CH, halogenated (F, Cl, Br, I) lower C ₂ -C ₆ alkynyl, lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I ) lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R',

where R 'represents, optionally, substituted alkyl, including, but not limited to, optionally substituted C _1-20 alkyl, optionally substituted C _1-10 alkyl, optionally substituted lower alkyl; possibly containing substituents cycloalkyl; possibly containing substituents with C ₂ -C ₆ alkynyl, possibly containing substituents with lower C ₂ -C ₆ alkenyl, or optionally containing acyl substituents, including but not limited to C (O) alkyl, C (O) (C _1-20 alkyl), C (O) (C _1-10 alkyl), or C (O) (lower alkyl), or, alternatively, in the case of NR ′ ₂ , each R ′ contains at least one C atom combined to form a heterocycle comprising at least two carbon atoms; and

R ¹² represents H, halogen (including F, Cl, Br, I), OH, OR ', SH, SR', NH ₂ , NHR ', NR' ₂ , NO ₂ lower alkyl C ₁ -C ₆ halogenated ( F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower alkynyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkynyl C ₂ -C ₆ , lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R'; with the proviso that when the base is represented by a structure where R ¹¹ is hydrogen, R ^{12 is} not: (i) —C≡C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

DEFINITIONS

When used in this description of the invention, the singular in relation to h / l may mean either one object or more; for example, a compound refers to one or more compounds, or to at least one compound. Also, the terms “one or more”, “at least one” may be used interchangeably herein.

The phrase "as defined above" refers to the first definition given in the presentation of the Summary of the Invention.

The terms “possible” or “maybe” used in the present description mean that the event or circumstance described below may not occur, and the description includes examples in which the event or circumstance is present, and examples in which the event or circumstance is not occurs. For example, “possible bond” means that the bond may not be present, and that the description includes single, double or triple bonds.

The term “independently” is used in the present description to indicate that the variable is used in any other example, regardless of the presence or absence of the same defined variable within the same connection. For example, in a compound in which R is used twice and is defined as “independently carbon or nitrogen”, both R may be carbon, both R may be nitrogen, or one R ’may be carbon and the other nitrogen.

The term "alkenyl" refers to a radical represented by a unsubstituted hydrocarbon chain of 2-10 atoms having one or two olefinic double bonds, preferably one olefinic double bond. The term "C _2-N alkenyl" refers to an alkenyl containing from 2 to N carbon atoms, where N is an integer that can take the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term " C _2-10 alkenyl "refers to alkenyl containing from 2 to 10 carbon atoms. The term “C _2-4 alkenyl” refers to alkenyl containing from 2 to 4 carbon atoms. Examples include, but are not limited to vinyl, 1-propenyl, 2-propenyl (allyl), or 2-butenyl (crotyl).

The term “halogenated alkenyl” refers to an alkenyl containing at least one of: F, Cl, Br, and I.

The term “alkyl” refers to a monovalent hydrocarbon residue represented by a straight or branched chain saturated containing from 1 to 30 carbon atoms. The term "C _1-M alkyl" refers to alkyl containing from 1 to M carbon atoms, where M is an integer that can take the following meanings: 2, 3, 4, 5, 6.7, 8, 9, 10.11 , 12,13,14,15,16,17, 18,19, 20, 21, 22,23, 24, 25, 26, 27, 28, 29, or 30. The term "C _1-4 alkyl" refers to alkyl containing from 1 to 4 carbon atoms. The term "lower alkyl" means a hydrocarbon residue represented by a straight or branched chain containing from 1 to 6 atoms. “C _1-20 alkyl,” as used herein, refers to alkyl containing from 1 to 20 carbon atoms. “C _1-10 alkyl,” as used herein, refers to alkyl containing from 1 to 10 carbon atoms. Examples of alkyl groups include, but are not limited to lower alkyl groups, including methyl, ethyl, propyl, iso-propyl, n-butyl, iso-butyl, tert-butyl or pentyl, isopentyl, neopentyl, hexyl, heptyl, and octyl. The term (ar) alkyl or (heteroaryl) alkyl means an alkyl group optionally substituted with an aryl or heteroaryl group, respectively.

The term "cycloalkyl" refers to a substituted or non-substituted carbocycle, wherein the carbocycle contains from 3 to 10 carbon atoms; preferably 3 to 8 carbon atoms; more preferably 3 to 6 carbon atoms (i.e. lower cycloalkyls). Examples of cycloalkyl groups include, but are not limited to cyclopropyl, 2-methyl-cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl.

The term “cycloalkylalkyl” refers to an additionally substituted or non-substituted alkyl containing lower cycloalkyl as a substitute. Examples of cycloalkyl alkyls include, but are not limited to any of the following: methyl, ethyl, propyl, iso-propyl, n-butyl, iso-butyl, t-butyl or pentyl, isopentyl, neopentyl, hexyl, heggal, and octyl containing as substituents cyclopropyl, 2-methylcyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl.

The term “cycloheteroalkyl” refers to a substituted or non-substituted heterocycle made up of 2-9 carbon atoms, preferably 2-7 carbon atoms, most preferably 2-5 carbon atoms. Examples of cycloheteroalkyls include, but are not limited to: aziridin-2-yl, N — C _1-3 -alkyl-aziridin-2-yl, azetidinyl, N — C _1-3 -alkyl-azetidin-m'-yl, pyrrolidin- m'-yl, N-C _1-3 -alkyl-pyrrolidin-m'-yl, piperidin-m'-yl, and N-C _1-3 -alkyl-piperidin-m'-yl, where m 'is 2 , 3, or 4 depending on cycloheteroalkyl. Specific examples of NC _1-3 -alkyl-cycloheteroalkyls include, but are not limited to: N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl -pyrrolidin-4-yl, N-methyl-piperidin-2-yl, N-methyl-piperidin-3-yl, and N-methyl-piperidin-4-yl. In the case of R ⁴ , the attachment point of oxygen to the carbon of the cycloheteroalkyl ring is in any of m.

The term “heterocycle” refers to a substituted or non-substituted heterocycle consisting of carbon, hydrogen, and at least one of the following: N, O, and S, where C and N may be trivalent or tetravalent, i.e. sp ² or sp ^{3 are} hybridized. Examples of heterocycles include, but are not limited to: aziridine, azetidine, pyrrolidine, piperidine, imidazole, oxazole, piperazine, etc. In the case of piperazine, when R ¹⁰ is NR ′ ₂ , the corresponding opposite nitrogen atom of piperazinyl has a substituent represented by lower alkyl, as shown in the formula:

.

.

A preferred substituent on the opposite nitrogen atom of piperazinyl is a methyl group.

The term “halogenated alkyl” (or “haloalkyl”) refers to straight or branched chain alkyl containing at least one of the following: F, Cl, Br, and I. The term “C _1-M haloalkyl” refers to an alkyl consisting of from 1 to M carbon atoms containing at least one of the following: F, Cl, Br and I, where M is an indicator that can take the following values: 2, 3, 4, 5, 6, 7, 8, 9 , 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, or 30. "C _1-3 haloalkyl "refers to haloalkyl containing from 1 to 3 carbon atoms and at least one of the following s: F, Cl, Br, and I. The term “halogenated lower alkyl” (or “lower haloalkyl”) refers to haloalkyl containing from 1 to 6 carbon atoms and at least one of the following: F, Cl, Br, and I. Examples include but are not limited to the following: fluoromethyl, chloromethyl, iodomethyl, difluoromethyl, dichloromethyl, dibromomethyl, diiodomethyl, trifluoromethyl, trichloromethyl, tribromomethyl, triiodomethyl, 1-fluoroethyl, 1-chloroethyl, 1-bromoethyl, 1-iodomethane fluoroethyl, 2-chloroethyl, 2-bromoethyl, 2-iodoethyl, 2,2-difluoroethyl, 2,2-dichloroethyl, 2,2-dibromomethyl, 2-2-diiodomethyl, 3-fluoropropyl, 3-chloropropyl, 3-bro mpropyl, 2,2,2-trifluoroethyl or 1,1,2,2,2-pentafluoroethyl.

The term "alkynyl" refers to a radical represented by a straight or branched hydrocarbon chain containing from 2 to 10 carbon atoms, preferably from 2 to 5 carbon atoms, and having one triple bond. The term "C _2-N alkynyl" refers to an alkynyl containing from 2 to N carbon atoms, where N is an indicator that can take the following values: 3, 4, 5, 6, 7, 8, 9, or 10. The term " C _2-4 alkynyl "refers to an alkynyl containing from 2 to 4 carbon atoms. The term “C _2-10 alkynyl” refers to an alkynyl containing from 2 to 10 carbon atoms. Examples include, but are not limited to, ethynyl, 1-propynyl, 2-propynyl, 1-butynyl, 2-butynyl, or 3-butynyl.

The term "halogenated alkynyl" refers to a radical represented by a straight or branched hydrocarbon chain containing from 2 to 10 carbon atoms, preferably from 2 to 5 carbon atoms, having one triple bond and containing at least one of the following: F, Cl, Br , and I.

The term "cycloalkyl" refers to a saturated carbocycle containing from 3 to 8 carbon atoms, i.e. cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl or cyclooctyl. The term “C _3-7 cycloalkyl,” as used herein, refers to cycloalkyl containing from 3 to 7 carbon atoms in a carbocycle.

The term “alkoxy” refers to an —O-alkyl group or to an —O-cycloalkyl group, wherein the definitions of alkyl and cycloalkyl are given above. Examples of —O-alkyl groups include, but are not limited to: methoxy, ethoxy, n-propyloxy, iso-propyloxy, n-butyloxy, iso-butyloxy, thi-butyloxy. The term “lower alkoxy” as used herein means an alkoxy group with a “lower alkyl” group as defined above. “C _1-10 alkoxy” refers to an —O-alkyl group, wherein alkyl refers to C _1-10 . Examples of —O-cycloalkyl groups include, but are not limited to, —O-c-propyl, -O-c-butyl, -O-c-pentyl, and -O-c-hexyl.

The term “halogenated alkoxy” refers to an —O-alkyl group that contains at least one of the following: F, Cl, Br and I.

The term “halogenated lower alkoxy” refers to an —O— (lower alkyl) group containing at least one of the following: F, Cl, Br, and I.

The term "amino acid" includes naturally occurring and synthesized α, β γ or δ amino acids, and includes, but is not limited to, amino acids found in proteins, i.e. glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, series, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate, lysine, arginine and histidine. A preferred embodiment are amino acids in the L configuration. Alternatively, the amino acid may be a derivative of alanyl, valinyl, leucinyl, isoleucinyl, proinyl, phenylalaniline, tryptophanyl, methioninyl, glycinyl, serynyl, threoninyl, cysteinyl, tyrosinyl, asparaginyl, glutaminyl, aspartoyl, glutaroyl, lisinyl vinyl ariline , β-valinyl, β-leucinyl, β-isoleucinyl, β-proline, β-phenylalaniline, β-tryptophanyl, β-methioninyl, β-glycinyl, β-serynyl, β-threoninyl, β-cysteinyl, β-tyrosinyl, β Asparaginyl, β-glutaminyl, β-aspartoyl, β-glutaroyl, β-lysinyl, β-arginine sludge or β-histidinyl. When using the term amino acid, they mean the specific and independent disclosure of each of the esters of α, β γ or δ glycine, alanine, valine, leucine, isoleucine, methionine, phenylalanine, tryptophan, proline, serine, threonine, cysteine, tyrosine, asparagine, glutamine, aspartate, glutamate , lysine, arginine and histidine in the D and L configurations.

The term “aminoacyl” includes N, N-not containing substituents, N, N-containing one Deputy, and N, N-disubstituted derivatives of natural and synthesized α, β γ or δ aminoacyls, where aminoacyls are derived from amino acids. The amino group nitrogen may or may not contain substituents. When the nitrogen of the amino group contains substituents, there may be one or two substituents, and such a substituent bound to the nitrogen of the amino group may be lower alkyl or alkaryl. If used for Y, the expression "O (aminoacyl)" is used. It is understood that the C3 ’ribose carbon atom is bonded to oxygen“ O ”, which, in turn, is bonded to the carbonyl carbon atom of the aminoacyl.

The term “alkylamino” or “arylamino” refers to an amino group containing one or two alkyl or aryl substituents, respectively.

The term "protected" used in the present description, unless otherwise specified, refers to a group attached to an oxygen, nitrogen or phosphorus atom to prevent its further interaction, or for other purposes. A wide range of oxygen and nitrogen protecting groups is known to those skilled in the art of organic synthesis. Non-exhaustive examples include: C (O) -alkyl, C (O) Ph, C (O) aryl, CH ₃ , CH ₂ -alkyl, CH ₂ -alkenyl, CH ₂ Ph, CH ₂ -aryl, CH ₂ O- alkyl, CH ₂ O-aryl, SO ₂ -alkyl, SO ₂ -aryl, tert-butyldimethylsilyl, tert-butyldiphenylsilyl, and 1,3- (1,1,3,3-tetraisopropyldisiloxanilidene).

The term “aryl” as used herein, unless otherwise specified, refers to phenyl (Ph), biphenyl, or naphthyl containing or not substituting, preferably, the term aryl is used to refer to phenyl containing or not containing substituents. The aryl group may contain one or more of the following functional groups as substituents: hydroxyl, F, Cl, Br, I, amino, alkylamino, arylamino, alkoxy, aryloxy, nitro, cyano, sulfonic acid, sulfate, phosphoric acid, phosphate and phosphonate which, if necessary, can be protected using methods known to specialists in this field of technology, for example, as shown in TW Greene and P.G. M. Wuts, "Protective Groups in Organic Synthesis," 3rd ed., John Wiley & Sons, 1999.

The term “alkaryl” or “alkylaryl” refers to an alkyl group containing an aryl substituent, for example benzyl. The terms “aralkyl” or “aryl alkyl” refer to an aryl group containing an alkyl substituent.

The term "di (lower alkyl) amino lower alkyl" refers to lower alkyl containing an amino group as a substituent, which, in turn, contains two lower alkyl substituents. Examples include, but are not limited to the following groups: (CH ₃ ) ₂ NCH ₂ , (CH ₃ ) ₂ NCH ₂ CH ₂ , (CH ₃ ) ₂ NCH ₂ CH ₂ CH ₂ , etc. The examples above demonstrate lower alkyls containing an N, N-dimethyl amino substituent at the terminal carbon atom. They are given in the present description solely as examples, and are not exhaustive meanings for the term "di (lower alkyl) amino lower alkyl". It is contemplated that the lower alkyl hydrocarbon chain may contain, as a substituent, an N, N-di (lower alkyl) amino group at any point in the chain, for example, CH ₃ CH (N- (lower alkyl) ₂ ) CH ₂ CH ₂ .

The term “halo” as used herein includes chloro, bromo, iodo and fluoro.

The term “acyl” refers to a substituent containing carbonyl and non-carbonyl functional groups. The carbonyl functional group contains a double bond between the carbonyl carbon atom and the heteroatom, where the heteroatom is selected from O, N and S. When the heteroatom is N, N has a lower alkyl substituent. Non-carbonyl functional group selected from the following: straight, branched, and cyclic alkyl including, but not limited to: straight, branched, or cyclic C1- ₂₀ alkyl, _C1-10 alkyl, or lower alkyl; alkoxyalkyl, including methoxymethyl; aralkyl, including benzyl; aryloxyalkyl, for example phenoxymethyl; or aryl including phenyl optionally having halogen as a substituent (F, Cl, Br, I ), hydroxy, alkyl from C ₁ to C 4, or C ₁ to C ₄ alkoxy, sulfonate esters such as alkyl or aralkyl sulfonyl, including methanesulfonyl, mono-, di- or triphosphate esters, trityl or monomethoxytretyl, benzyl containing substituents, trialkylsilyl (e.g. dimethyl-t-butylsilyl) or diphenylmethylsilyl. When at least one aryl group is present in a non-carbonyl functional group, it is preferred that the phenyl group is such an aryl group.

The term “lower acyl” refers to an acyl group in which the non-carbonyl functional group is lower alkyl.

The term "purine" or "pyrimidine" base includes, but is not limited to: adenine, N ⁶ -alkylpurines, N ^6- acylpurines (where acyl is C (O) (alkyl, aryl, alkylaryl, or arylalkyl), N ⁶ - benzylpurine, N ⁶ -galopurin, N ^6- vinylpurine, N ⁶ -acetylene purine, N ⁶ -acyl purine, N ⁶ -hydroxyalkyl purine, N ^6- allylaminopurine, N ⁶ -thioallylpurine, N ² -alkylpurines, N ² -alkyl- 6-thiopurines, thymine, cytosine, 5-fluorocytosine, 5-methylcytosine, 6-azapyrimidines, including 6-azacytosine, 2- and / or 4-mercaptopyrimidine, uracil, 5-galouratsil, including 5-fluorouracil, C ⁵ -alkenes pyrimidines -benzilpirimidiny C ^5, C ⁵ -galopirimidiny, -vinilpirimidin C ^5, C ⁵ -atsetilenovy pyrimidine, C ⁵ -acyl pyrimidine, C ⁵ -hydroxyalkyl purine, C ⁵ -amidopirimidin, -tsianopirimidin C ^5, C ⁵ -yodpirimidin, -yodpirimidin C ^6, C ⁵ -Br-vinyl pyrimidine, C ⁶ -Br-vinyl pyrimidine, C ⁵ -nitropirimidin, C ⁵ -aminopirimidin, N -alkilpuriny ^2, N ² -alkyl-6-thiopurines, 5-azacytidine, 5 α-azauracidyl, triazolopyridinyl, imidazole pyridinyl, pyrrolopyrimidinyl, and pyrazolopyrimidinyl. Purine bases include, but are not limited to: guanine, adenine, hypoxanthine, 2,6-diaminopurin, and 6-chloropurine. Functional oxygen and nitrogen groups of the base can be protected if necessary or optional. Suitable protecting groups for this are known to those skilled in the art and include trimethylsilyl, dimethylhexylsilyl, t-butyldimethylsilyl, and t-butyldiphenylsilyl, trityl, alkyl groups, and acyl groups, for example, acetyl and spionyl, methanesulfonyl, and p-toluenesulfon.

The terms "tautomerism" and "tautomers" correspond to generally accepted meanings.

The term "P *" means that the phosphorus atom has chirality and has the corresponding designation according to the Kahn-Ingold-Prelog system "R" or "S", which correspond to generally accepted values. The compounds of formula I are believed to be racemic mixtures due to the chirality of the phosphorus atom. Applicants contemplate the use of racemate and / or resolved enantiomers. In some cases, an asterisk is missing near the phosphoramidate phosphorus atom. In such cases, it is understood that the phosphorus atom has chirality, and it is obvious to a person skilled in the art that this is so if phosphorus-related substituents do not exclude the possibility of chirality, as is the case for P (O) Cl ₃ .

DETAILED DESCRIPTION OF THE INVENTION

According to one aspect, the present invention provides a compound, its salts, hydrates, solvates, crystalline forms, etc., represented by formula I:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl or naphthyl, where phenyl or naphthyl may contain at least one of a number of substituents: alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _1-6 alkoxy, F , Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, —N (R ^{1 ′} ) ₂ , acylamino, —NHSO ₂ C _1-6 alkyl, —SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ''} and -SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' represents -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen, C _1-10 alkyl, R ^3a or R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms, C (O) CR ^3a R ^3b NHR ¹ , where n is from 2 to 4 and R ¹ , R ^3a , and R ^3b ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) C (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ^{3 ″} , aryl and aryl C _1-3 alkyl, said aryl groups may contain a substituent selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed comprising neighboring N and C atoms, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3, f is from 2 to 5, n is from 2 to 4, and where R3 is independently hydrogen or C _1-6 alkyl and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) —Ph), CH ₂ SH, or lower cycloalkyl and R ^3b is H, where R ^{3 ′ is} independently hydrogen or alkyl, including but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _{1- 6 by} alkyl, R ^{3 ″} or —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, optionally having a substituent from the series: lower alkyl, alkoxy, di (lower alkyl) amino, or hydrogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl such as phenyl, heteroaryl such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxyl lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including methyl hydroxyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) represents H, OH, F, OMe, halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OC (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-10 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , N (C _1-18 acyl) ₂ , where alkyl, alkynyl alkenyl and vinyl, in possibly contain as substituent N ₃ , CN, from one to three halogens (Cl, Br, F, I), NO ₂ , C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _2-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , N (C _1-4 acyl) ₂ ;

the base, by its nature, belongs to modified purine or pyrimidine bases, represented by the following structures:

Where

Z represents N or CR ¹² ;

R ⁷ , R ⁸ , R ⁹ , R ¹⁰ , and R ¹¹ independently represent H, F, Cl, Br, I, OH, OR ', SH, SR', NH ₂ , NHR ', NR' ₂ , lower alkyl C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated
lower (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower alkynyl C ₂ -C ₆ , such as C = CH, halogenated (F, Cl, Br, I) lower alkynyl of C ₂ -C ₆ , lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ N, or CH = CHCO ₂ R ',

where R 'is optionally substituted alkyl, including, but not limited to, optionally substituted C _1-20 alkyl, optionally substituted C _1-10 alkyl, optionally lower alkyl; possibly containing substituents cycloalkyl; possibly containing substituents with C ₂ -C ₆ alkynyl, possibly containing substituents with lower C ₂ -C ₆ alkenyl, or optionally containing acyl substituents, including but not limited to C (O) alkyl, C (O) (C _1-20 alkyl), C (O) (C _1-10 alkyl), or C (O) (lower alkyl) or, alternatively, in the case of NR ′ ₂ , each R ′ contains at least one C atom combined to form a heterocycle comprising at least two carbon atoms; and

R ¹² represents H, halogen (including F, Cl, Br, I), OH, OR ', SH, SR', NH ₂ , NHR ', NR' ₂ , NO ₂ lower alkyl C ₁ -C ₆ halogenated ( F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower alkynyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkynyl C ₂ -C ₆ , lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R'; with the proviso that when the base is represented by a structure where R ¹¹ is hydrogen, R ^{12 is} not: (i) —C≡C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

As can be understood from the structure presented above in Formula I, there are myriads of ways to map several embodiments of the present invention and aspects of each embodiment of the present invention. As will be seen below, the inventors have discovered several options for the implementation of the compounds of formula I, each of which has several aspects based on the characteristics of the modified purine or pyrimidine base. This is not a direct or indirect indication that the above compounds are independent or different, and this should not be interpreted in this way. Rather, it is intended to convey information in such a way that the full scope of the present invention can be understood. Moreover, the full scope of the invention is not limited to the following implementation options and aspects thereof, as shown by the structure of formula I.

According to a first embodiment of the invention, there is provided a compound represented by formula 1-1:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to, phenyl or naphthyl, where phenyl or naphthyl may contain at least one of a number of substituents: C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1 -6} alkoxy, F, Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen, C _1-10 alkyl, R ^3a or R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms, C (O) CR ^3a R ^3b NHR ¹ , where n is from 2 to 4 and R ¹ , R ^3a , and R ^3b ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) _c (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ³ ″, aryl and aryl C _1-3 alkyl, said aryl groups may contain a substituent selected from hydrogen, C _1-10 alkyl, alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3, f is from 2 to 5, n is from 2 to 4, and where R ^{3 ′ is} independently hydrogen or C _1-6 alkyl and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazole 1-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) —Ph), CH ₂ SH, or lower cycloalkyl and R ^3b is H, where R ³ ′ is independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _{1- 6 by} alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, optionally having a substituent from the series: lower alkyl, alkoxy, di (lower alkyl) amino, or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl such as phenyl, heteroaryl such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OC (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _2-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , N (C _1-18 acyl) ₂ , where alkyl, alkynyl alkenyl and vinyl maybe contain as substituents N ₃ , CN, from one to three halogens (Cl, Br, F, I), NO ₂ , C (O) O (C _1-4 alkyl), C (O) O (C _1-4 alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl) , SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _2-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl1), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ ( C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _2-4 acyl), N (C _{1 -4} alkyl) ₂ , N (C _1-4 acyl) ₂ ;

(i) R ⁷ , R ⁸ , R ⁹ independently represent H, F, Cl, Br, I, OH, OR ′, SH, SR ′, NH ₂ , NHR ′, NR ′ ₂ , lower alkyl, halogenated (F , Cl, Br, I) lower alkyl, lower alkenyl C ₂ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , where R' is C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a first aspect of a first embodiment of the invention, there is provided a compound represented by formula I-1

Where

(a) R ¹ is hydrogen, n-alkyl or aryl, including but not limited to phenyl or naphthyl, wherein phenyl or naphthyl may contain, as substituents, at least one from the group of C ₁ - ₆ alkyl, C ₁ - ₆ alkoxy, F, Cl, Br, I, nitro, cyano, C ₁ - ₆ haloalkyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b independently (i) R ^3a represents hydrogen and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed that includes adjacent N and C atoms, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3, f is from 3 to 5, n is early from 2 to 4, and where R ^{3 ′ is} independently hydrogen or C _1-6 alkyl and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ) ; (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ СОН, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazole 1-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), or CH ₂ SH and R ^3b represents H;

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, optionally having substituents lower alkyl, alkoxy, di (lower alkyl) amino, or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl, aminoacyl, aryl such as phenyl, heteroaryl such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ represents H, CN, CH ₃ , vinyl, OCH ₃ , OCH ₂ CH ₃ , CH ₂ OH, CH ₂ (halo), such as CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine, and R ⁶ represents H; R ⁵ cannot be N ₃ ;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, vinyl, N ₃ , CN, Cl, Br, F, I, O (C _1-6 acyl), O (C _1-4 alkyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _2-4 acyl), N (C _1-4 alkyl) ₂ , N ( C _1-18 acyl) ₂ , where alkyl, alkenyl, alkynyl and vinyl may optionally contain N ₃ , CN, one to three halogens (Cl, Br, F, I), NO ₂ , OS (O) as substituents O (C _1-4 alkyl) OC (O) O (C _1-4 alkyl) OC (O) O _(C2-4 alkynyl), OC (O) O _(C2-4 alkenyl) OC _{1 -4} haloalkyl, O (aminoacyl), O (C _1-4 acyl1), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl1), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl1) ₂ , or N (C _1-4 acyl) ₂ ;

(i) R ⁷ , R ⁸ , R ⁹ independently represent H, F, Cl, Br, I, OH, OR ', SH, SR', NH ₂ , NHR ', NR' ₂ , lower alkyl, halogenated (F , Cl, Br, I) lower alkyl, lower alkenyl from the series: C ₂ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , where R' represents C _1-20 alkyl ; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a second aspect of the first embodiment of the invention, there is provided a compound of formula I-1

Where

(a) R ¹ represents hydrogen, n-alkyl, or phenyl containing or not containing substituents, where the substituent in the phenyl containing such is at least one of the series: C _1-3 alkyl, C _1-3 alkoxy, F, Cl , Br, I, nitro, cyano, and C _1-3 haloalkyl;

(b) R ₂ represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b independently (i) R ^3a represents hydrogen and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed that includes adjacent N and C atoms, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3, f is from 3 to 5, n early from 2 to 4, and where R3 independently is hydrogen or C _1-6 alkyl and R3 “is —OR” or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ ) -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), or CH ₂ SH and R ^3b represents H;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl, or aminoacyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ (halo), such as CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ^{5 is} not may be N ₃ ;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ ; and

(j) R ^{9 is} selected from OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , OC (O) (C _1-20 alkyl), including but not limited to OC (O ) (CH ₂ ) _s CH ₃ , NHC (O) (C _1-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , including but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , where s is an integer selected from: 0, 1, 2, 3, 4, 5, 6, 7 , 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to a third aspect of the first embodiment of the invention, there is provided a compound of formula I-1

Where

(a) R ¹ represents hydrogen, n-alkyl, or phenyl containing or not containing substituents, where the substituent in the phenyl containing such is at least one of the series: CH ₃ , OCH ₃ , F, Cl, Br, I, nitro , cyano, and CH _3-q X _q , where X is F, Cl, Br, or I, and q is 1-3;

(b) R represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl, or R ^3a represents CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph , CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4 '-OH) -Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b represents H;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl, or aminoacyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ (halo), such as CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R6 is H, R ⁵ cannot be N ₃ ;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, O, Br, or I, and q is from 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ , where R 'represents C _1-20 alkyl 1; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl '; and

(j) R ^{9 is} selected from: OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , OC (O) (C _1-20 alkyl), including but not limited to OC ( O) (CH ₂ ) _s CH ₃ , NHC (O) (C _l-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , including but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , where s is an integer selected from: 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to a fourth aspect of the first embodiment of the invention, there is provided a compound represented by Formula I-2:

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, or substituted or unsubstituted phenyl, or phenyl containing or not containing substituents, where the substituent in the phenyl containing them is at least one substituent from the series: CH ₃ , OCH ₃ , F, Cl, Br, I, nitro, cyano and CH _3-q X _q , where X is F, C1, Br, or I, and q is 1-3;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl, or R ^3a represents CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph , CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4 '—OH) —Ph), CH ₂ SH or lower cycloalkyl, and R is H;

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R5 is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N ( CH ₃ ) 2, halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ ;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, Cl, Br, or I, and q is from 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ , where R 'represents C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl; and

(j) R ^{9 is} selected from: OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , OC (O) (C _1-20 alkyl), including but not limited to OC ( O) (CH ₂ ) _s CH ₃ , NHC (O) (C _1-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) _s CH ₃ , including but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) 2, where s is an integer selected from: 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to a fifth aspect of a first embodiment of the invention, there is provided a compound represented by Formulas 1-2

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R represents hydrogen or CH ₃ ;

(c) R ^3a is H and R ^3b is H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -irmidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl, or aminoacyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, O, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, O, Br, or I, and q is 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ , where R 'represents C _1-20 alkyl; C _1-20 cycloalkyl1; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl; and

(j) R ^{9 is} selected from: OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , OC (O) (C _1-20 alkyl), including but not limited to OC ( O) (CH ₂ ) _s CH ₃ , NHC (O) (C _1-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , including but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , where s is an integer selected from: 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to a sixth aspect of a first embodiment of the invention, there is provided a compound represented by formula I-2

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ represents H, OMe, CN, CH ₂ F, F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, or N ₃ , OCH ₃ , OC (O) CH ₃ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Br, SCH ₃ , CH ₃ , CH _3-q X _q , where X represents F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ ; and

(j) R ^{9 is} selected from OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , OC (O) (C _1-20 alkyl), including but not limited to OC (O ) (CH ₂ ) _s CH ₃ , NHC (O) (C _1-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) SCH ₃ ) ₂ , including but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , where s is an integer selected from 0, 1, 2, 3, 4, 5, 6, 7, 8 , 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to a seventh aspect of a first embodiment of the invention, there is provided a compound represented by formula 1-2

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) 2, CH ₂ CH (CH ₃ ) 2, CH (CH ₃ ) CHrCH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, or N ₃ ;

(h) Y represents OH, OCH ₃ , OC (O) CH ₃ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Br, SCH ₃ , CH ₃ , CH _3-q X _q , where X is F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ ; and

(j) R ^{9 is} selected from: OH, OCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) 2, OC (O) (C _1-20 alkyl), including but not limited to OC (O) (CH ₂ ) sCH ₃ , NHC (O) (C _1-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) sCH ₃ ) ₂ , including but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , where s is an integer selected from: 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10 , 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to an eighth aspect of a first embodiment of the invention, there is provided a compound represented by Formula I-2

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, K-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, or N ₃ ;

(h) Y represents OH, OCH ₃ , OC (O) CH ₃ , or O (aminoacyl);

(i) R ⁷ and R ⁸ independently represent H, F, Br, SCH ₃ , CH ₃ , CH _3-q X _q , where X represents F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ ;

(j) R ^{9 is} selected from: OH, OCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , OC (O) (C _1-20 alkyl), including but not limited to OS (O) (CH ₂ ) _s CH ₃ , NHC (O) (C _1-20 alkyl), including but not limited to NHC (O) (CH ₂ ) _s CH ₃ , and N (C (O) (CH ₂ ) _s CH ₃ ) ₂ including, but not limited to N (C (O) (CH ₂ ) _s CH ₃ ) ₂ , where s is an integer selected from: 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 , 10, 11, 12, 13, 14, 15, 16, 17, 18, and 19.

According to a second embodiment of the invention, there is provided a compound represented by Formula I, wherein the base is the structure represented by Formula b, R ¹ , R ² , R ^3a , R ^3b , R ⁴ , R ⁵ , R ⁶ , X, Y, R ⁷ and R ^{8 are} defined in the Summary of the Invention.

According to a first aspect of a second embodiment of the invention, there is provided a compound represented by formula I-3:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthyl, where phenyl and naphthyl may optionally contain at least one of the series C _1-6 alkyl, C _2-6 alkenyl 1, C _2-6 alkynyl, C _{1 -6} alkoxy, F, O, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acyamino, -NHSO ² C _1-6 alkyl, -SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) C (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - (CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ^{3 ''} , aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano ; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5, n is early from 2 to 4, and where R ^{3 ′ is} independently hydrogen or C _1-6 alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , sn ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Sh, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO2H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph ), CH ₂ SH, or lower cycloalkyl, and R ^3b represents H, where R independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl, containing substituents, or heteroaryl, containing substituents;

(e) R ⁵ represents H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e., - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F , Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R6 is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F and B represents a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OC (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-10 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _2-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) 2, or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, in Possible contain as substituent N _3, CN, one to three halogen (Cl, Br, F, I ), NO _2, C (O) O (C _1-4 alkyl), C (O) O ( C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , or N (C _1-4 acyl) ₂ ;

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OR ′, SH, SR ′, NH ₂ , NHR ′, NR ′ ₂ , lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl C ₂ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , where R' represents C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a second aspect of a second embodiment of the invention, there is provided a compound represented by formula I-3

Where

(a) R ¹ R ¹ represents hydrogen, n-alkyl or aryl, including but not limited to phenyl or naphthyl, where phenyl or naphthyl may contain at least one of a number of substituents: alkyl, alkoxy, F, Cl , Br, I, nitro, cyano, haloalkyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b independently (i) R ^3a represents hydrogen and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed that includes adjacent N and C atoms, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3, f is from 3 to 5, n is early from 2 to 4, and where R is independently hydrogen or C _1-6 alkyl and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ СОН, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazole 1-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), or CH ₂ SH and R ^3b represents H;

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ represents H, CN, CH ₃ , vinyl, OCH ₃ , OCH ₂ CH ₃ , CH ₂ OH, CH ₂ (halo), such as CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, vinyl, N ₃ , CN, Cl, Br, F, I, O (C _1-6 acyl), O (C _1-4 alkyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , N ( C _1-18 aiyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl may optionally contain as substituents N ₃ , CN, one to three halogens (Cl, Br, F, I), NO ₂ , OC (O) O (C _1-4 alkyl), OS (O) O (C _1-4 alkyl), OS (O) O (C _2-4 alkynyl), OS (O) O (C _2-4 alkenyl), OS _{1 -10} haloalkyl, O (aminoacyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl, S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO ( C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl) , SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O ) 2 (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _2-4 acyl), N (C _1-4 alkyl) ₂ , N (C _1-4 acyl) ₂ ;

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OR ′, SH, SR ′, NH ₂ , NHR ′, NR ′ ₂ , lower alkyl, halogenated (F, Cl, Br, I) lower alkyl, lower alkenyl C ₂ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , where R' represents C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a third aspect of a second embodiment of the invention, there is provided a compound represented by formula I-3

Where

(a) R ¹ represents hydrogen, n-alkyl, or phenyl containing or not containing substituents, where the substituent in the phenyl containing such is at least one of the series: CH ₃ , OCH ₃ , F, Cl, Br, I, nitro , cyano, and d-3 haloalkyl;

(b) R ² represents hydrogen, CH ₃ , R ^3a or R ^3b and R ² together represent (CH ₂ ) ₃ such that a cyclic ring is formed comprising adjacent N and C atoms, C (O) CR ^3a R ^3b NHR ¹ , where n is from 2 to 4 and R ¹ , R ^3a , and R ^3b are as defined above;

(c) R ^3a and R ^3b independently (i) R ^3a represents hydrogen R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b represents hydrogen and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed comprising adjacent N and C atoms, where c is from 1 to 6, d is from 0 to 2, e is from 0 to 3 , f is from 3 to 5, n is early from 2 to 4, and where R ^{3 ′} independently is C _1-6 alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO2H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) - Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b represents H;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ (halo), such as CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , halogen, NH ₂ , or N ₃

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ ;

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, Cl, Br, or I, and q is early 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ .

According to a fourth aspect of a second embodiment of the invention, there is provided a compound represented by formula I-3

Where

(a) R ¹ represents hydrogen, n-alkyl, or phenyl containing or not containing substituents, where the substituent in the phenyl containing such is at least one of the series: CH ₃ , OCH ₃ , F, Cl, Br, I, nitro , cyano, and CH _3-q X _q , where X is F, Cl, Br, or I, and q is I-3;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl, or R ^3a represents CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph , CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4 '-OH) -Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b represents H;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, Y-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, K-methyl-pyrrolidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ (halo), such as CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents, H, OH, F, OCH ₃ , NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ ;

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, Cl, Br, or I, and q is 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ , where R 'represents C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a fourth aspect of a second embodiment of the invention, there is provided a compound represented by formula I-4:

Where

(a) R ¹ represents hydrogen, n-alkyl, or phenyl containing or not containing substituents, where the substituent in the phenyl containing such is at least one of the series: CH ₃ , OCH ₃ , F, Cl, Br, I, nitro , cyano, and CH _3-q X _q , where X is F, Cl, Br, or I, and q is 1-3;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl, or R ^3a is CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ ) CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ ) -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4 ' —OH) —Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b represents H;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu 2-butyl, ^t Vi, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, K-methylaziridin-2-yl, N -methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ ;

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, Cl, Br, or I, and q is from 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ , where R 'represents C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a sixth aspect of a second embodiment of the invention, there is provided a compound represented by formula 1-4

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromophenyl, p-chlorophenyl, p-fluorophenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO2H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) - Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methylpiperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl ;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

(i) R ⁷ and R ⁸ independently represent H, F, Cl, Br, I, OH, OCH ₃ , SH, SCH ₃ , NH ₂ , NHCH ₃ , N (CH ₃ ) ₂ , CH ₃ , CH _{3- q} X _q , where X is F, Cl, Br, or I and q is 1 to 3, vinyl, CO ₂ H, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ , where R 'represents C _1-20 alkyl; C _1-20 cycloalkyl; C ₂ -C ₆ alkenyl; C ₂ -C ₆ alkynyl.

According to a seventh aspect of a second embodiment of the invention, there is provided a compound represented by formula I-4

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromophenyl, p-chlorophenyl, p-fluorophenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methylpiperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl ;

(e) R ⁵ represents H, OMe, CN, CH ₂ F, F, Cl, Br, or I;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , NOSH, or OS (O) CH ₃ ;

(i) R ⁷ and R ⁸ independently represent H, F, Br, SCH ₃ , CH ₃ , CH _3-q X _q , where X represents F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ ;

According to an eighth aspect of a second embodiment of the invention, there is provided a compound represented by formula I-4

Where

(a) R ¹ represents hydrogen, methyl, ethyl, l-propyl, i-propyl, phenyl, p-tolyl, p-bromophenyl, p-chlorophenyl, p-fluorophenyl;

(b) R ² represents hydrogen or;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R4 is hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N -methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF2, CF3, or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OS (O) CH ₃ ;

(i) R ⁷ and R ⁸ independently represent H, F, Br, SCH ₃ , CH ₃ , CH _3-q X _q , where X represents F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ .

According to a ninth aspect of a second embodiment of the invention, there is provided a compound represented by formula I-4

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N -methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, or N ₃ ;

(h) Y represents OH, OCH ₃ , or OS (O) CH ₃ ;

(i) R ⁷ and R ⁸ independently represent H, F, Br, SCH ₃ , CH ₃ , CH _3-q X _q , where X is F, Cl, Br, or I and q is from 1 to 3, vinyl, CO ₂ CH ₃ , CONH ₂ , CONHCH ₃ , or CON (CH ₃ ) ₂ .

According to a third embodiment of the invention, there is provided a compound represented by Formula I, wherein the base has the structure represented by Formula c above, a R ¹ , R ² , R ^3a , R ^3b , R ⁴ , R ⁵ , R ⁶ , X, Y Z, R ¹⁰ , R ¹¹ , and R ^{12 are} defined in the Summary of the Invention, provided that R ^{11 is} not H.

According to a first aspect of a third embodiment of the invention, there is provided a compound represented by formula 1-5:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthyl, where phenyl and naphthyl may optionally contain at least one of the series C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1 -6} alkoxy, F, O, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acyamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) _c (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - (CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR, aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5n early from 2 to 4, and where R ^{3 ′ is} independently hydrogen or C _1-6 alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b is H, where R ^{3 ′ is} independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, halogen, NH ₂ or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OC (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _2-4 acyl), OS (O) ₂ (C _2-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, in Possible contain as substituent N _3, CN, one to three halogen (Cl, Br, F, I ), NO _2, C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , or N (C _1-4 acyl) ₂ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Cl, Br, I, OH, OR ′, SH, SR ′, NH ₂ , NHR ′, NR ′ ₂ , lower alkyl C _1-6 , halogenated ( F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower alkynyl C ₂ -C ₆ , such as C≡CH, halogenated (F, Cl, Br, I) lower alkynyl C ₂ -C ₆ , lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R', with the proviso that when R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents alkyl, possibly containing substituents, including, but not limited to, C _1-20 alkyl, possibly containing substituents, C _1-10 alkyl, possibly containing substituents, lower alkyl, possibly containing substituents; cycloalkyl optionally containing substituents; C ₂ -C ₆ alkynyl, possibly containing substituents, C ₂ -C ₆ lower alkenyl, possibly containing substituents, or acyl, possibly containing substituents, including but not limited to C (O) alkyl, C (O) (C _1-20 alkyl), C (O) (C _1-10 alkyl), or C (O) (lower alkyl) or, as an alternative, in the case of NR ′ ₂ , each R ′ contains at least one C atom, which bind to form a heterocycle comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OH, OR ', SH, SR', NH ₂ , NHR ', NR' ₂ , NO ₂ lower alkyl C ₁ -C ₆ halogenated ( F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower alkynyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkynyl C ₂ -C ₆ , lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R'.

According to a second aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N -methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, Cl, Br, or I, with the proviso that when X is OH, R ⁶ is CH ₃ or CH ₂ F, R ⁵ cannot be N.

(f) R6 is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that when R ¹⁰ is OH and R ¹¹ cannot be NH ₂ ;

where R ¹ represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR ′ ₂ , each R ′ contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a third aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromophenyl, p-chlorophenyl, p-fluorophenyl;

(b) R represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N -methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₂ F, F, Cl, Br, or I; with the proviso that X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R6 is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that when R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, O, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, mhCH = CHCO ₂ R '.

According to a fourth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, No. methyl-aziridin-2-yl, N-methyl -azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl ;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that when R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

q) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a fifth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ¹ represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) 2, CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that when R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a sixth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chlorophenyl, p-fluorophenyl;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, K-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, O, Br, or I, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be N.

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a seventh aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₂ F, F, Cl, Br, or I; with the proviso that X represents OH, R6 represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R6 is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to an eighth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-5

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ is NH ₂ and R ¹¹ is H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or H = CHCO ₂ R '.

According to a ninth aspect of a third embodiment of the invention, there is provided a compound represented by Formula I-5

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R6 represents CH ₃ or CH ₂ F, R5 cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a tenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthyl, where phenyl and naphthyl may contain, as substituents, at least one of the series C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1 -6} alkoxy, F, Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) C (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ^{3 ’} , aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5, n is early from 2 to 4, and where R ³ independently is hydrogen or C _1-6 alkyl, and R ^{3 ′} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) —Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b is H, where R ^{3 ′ is} independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _{1 -6} alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F, and B is a purine base, R5 cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, POSSIBILITY contain as substituent N _3, CN, one to three halogen (Cl, Br, F, I ), NO _2, C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) 2 (C _1-4 alkyl), OS (O) 2 (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) 2, or N (C _1-4 acyl) ₂ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that when R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to an eleventh aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO2H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) - Ph), CH ₂ SH or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N- methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-metal-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, Cl, Br, or I, with the proviso that when X is OH, R ⁶ is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that when R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl of C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a twelfth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6,

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyppolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₂ F, F, O, Br, or I, with the proviso that when X is OH, R6 is CH ₃ or CH ₂ F, R ⁵ cannot be H ;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a thirteenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a fourteenth aspect of a third embodiment of the invention, there is provided a compound represented by formula 1-6

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl ;;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ independently represent H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ', with the proviso that R ¹⁰ is OH and R ^{11 is} not NH ₂ ;

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a fifteenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthyl, where phenyl and naphthyl may optionally contain at least one of the series C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1 -6} alkoxy, F, Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) C (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ₃ , aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5, n is early from 2 to 4, and where R3 is independently hydrogen or alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a represents CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) —Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b is H, where R ^{3 ′ is} independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _{1 -6} alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, O, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F, and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, halogen NH ₂ or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OC (O) O (C _1-4 alkyl), OC (O) O (C _2-4 alkynyl), OC (O) O (C _2-4 alkenyl), OC _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _1-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, in possibly contain as substituents N ₃ , CN, from one to three halogens (Cl, Br, F, I), NO ₂ , C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , or N (C _1-4 acyl) ₂ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a sixteenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, O, Br, or I, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a seventeenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₂ F, F, O, Br, or I, with the proviso that when X is OH, R ⁶ is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to an eighteenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ represents H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a nineteenth aspect of a third embodiment of the invention, there is provided a compound represented by formula I-6

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R4 is hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N -methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents NH ₂ and R ¹¹ independently represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z is N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a fourth embodiment of the invention, there is provided a compound represented by Formula I, wherein the base is the structure represented by Formula C above, wherein R ¹¹ is H and R ² , R ^3a , R ^3b , R ⁴ , R ⁵ , R ⁶ , X, and Y are defined in the summary of the "Summary of the Invention".

According to a first aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-7:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthyl, where phenyl and naphthyl may optionally contain at least one of a series of alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _1-6 alkoxy, F, Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N (R) ₂ , COR ^{1 ″} , and —SO ₂ Cn _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) _c (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ^{3 ''} , aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5n early from 2 to 4, and where R ^{3 ′ is} independently hydrogen or C _1-6 alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a is CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) —Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b is H, where R ^{3 ′ is} independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _{1 -6} alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, O, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F, and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OS (O) O (C _1-4 alkyl), OS (O) O (C _2-4 alkynyl), OS (O) O (C _2-4 alkenyl), OS _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) 2, or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, POSSIBILITY contain as substituent N _3, CN, one to three halogens (O, Br, F, I), NO _2, C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , or N (C _1-4 acyl) ₂ ;

(i) R ¹⁰ represents H, F, Cl, Br, I, OH, OR ', SH, SR', NH ₂ , NHR ', NR'2, C ₁ -C ₆ lower alkyl, halogenated (F, Cl , Br, I) lower alkyl C ₁ -C ₆ lower alkenyl, _C2-C6, halogenated (F, Cl, Br, I) lower alkenyl of C ₂ -C ₆ alkynyl nishy C ₂ -C ₆ such as С≡СН, halogenated (F, Cl, Br, I) lower alkynyl С ₂ -С ₆ , lower alkoxy C ₁ -С ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R', where R 'is alkyl, optionally containing substituents, including but not limited to C _{1 -20} alkyl, optionally substituted, C _1-10 alkyl, possibly containing substituents, lower alkyl, possibly containing substituents; cycloalkyl optionally containing substituents; C ₂ -C ₆ alkynyl optionally containing substituents, lower alkenyl C ₂ -C ₆ optionally containing substituents, or acyl optionally containing substituents, including but not limited to C (O) alkyl, C (O) (C _1-20 alkyl), C (O) (C _1-20 alkyl), or C (O) (lower alkyl) or, alternatively, in the case of NR ′ ₂ , each R ′ contains at least one C atom, which bind to form a heterocycle comprising at least two carbon atoms

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OH, OR ', SH, SR', NH ₂ , NHR ', NR' ₂ , NO ₂ lower alkyl C ₁ -C ₆ halogenated ( F, Cl, Br, I) lower alkyl C ₁ -C ₆ , lower alkenyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkenyl C ₂ -C ₆ , lower alkynyl C ₂ -C ₆ , halogenated (F, Cl, Br, I) lower alkynyl C ₂ -C ₆ , lower alkoxy C ₁ -C ₆ , halogenated (F, Cl, Br, I) lower alkoxy C ₁ -C ₆ , CO ₂ H, CO ₂ R ', CONH ₂ , CONHR', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R'; with the proviso that R ^{12 is} not: (i) —C = C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a second aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-7

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ СОН, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, O, Br, or I, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be N.

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ ) N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

(i) R ¹⁰ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that R ^{12 is} not: (i) —C = C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a third aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-7

Where

(a) R1 is hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ³ represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₂ F, F, Cl, Br, or I; with the proviso that X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR '', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that R ^{12 is} not: (i) —C = C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a fourth aspect of a fourth embodiment of the invention, there is provided a compound represented by Formula I-7

Where

(a) R ¹ represents hydrogen, methyl, ethyl, i-propyl, i-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ and R ¹¹ are H, F, Br, I, OH, OR ′, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that R ^{12 is} not: (i) —C = C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a fifth aspect of a fourth embodiment of the invention, there is provided a compound represented by Formula I-7

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H , or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '.

According to a sixth aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-8:

Where

(a) R ¹ represents hydrogen, n-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthol, where phenyl and naphthyl may optionally contain at least one of the series C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1 -6} alkoxy, F, O, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ^{1 '} ) ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N (R ^{1 ′} ) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 '} independently represents hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _1-6 alkyl, R ^1'' is -OR' or -N (R ^{1 '} ) ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) C (NR ^{3 '} ) ₂ , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ^{3 ″} , aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5n early from 2 to 4, and where R ^{3 ′ is} independently hydrogen or C _1-6 alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a represents CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b is H, where R ^{3 'is} independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F, and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OS (O) O (C _1-4 alkyl), OS (O) O (C _2-4 alkynyl), OS (O) O (C _2-4 alkenyl), OS _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, in possibly contain as substituents N ₃ , CN, from one to three halogens (Cl, Br, F, I), NO ₂ , C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _1-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , or N (C _1-4 acyl) ₂ ;

(i) R ¹⁰ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR '', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that when the base is represented by structure c, where R ¹¹ is hydrogen, R ^{12 is} not: (i) —C═CH — (ii) —C═CH ₂ , or (iii) —NO ₂ .

According to a seventh aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-8

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, shopropyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a is H and R ^3b is H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol -3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) - Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, O, Br, or I, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃

(i) R ¹⁰ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H or CH = CHCO ₂ R ';

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR '', CONR ' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R''; with the proviso that R ^{12 is} not: (i) —C≡C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to an eighth aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-8

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₂ F, F, Cl, Br, or I, with the proviso that when X - is OH, R ⁶ is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ is H, F, Br, I, OH, OR ″, NH ₂ , NHR ′, NR ′ ₂ , CO ₂ R ′, CONH ₂ , CONHR ′, CONR ′ ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that R ^{12 is} not: (i) —C = C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a ninth aspect of a fourth embodiment of the invention, there is provided a compound represented by formula I-8

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R10 represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, Cl, Br, I), OR ', NH ₂ , NHR', NR ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R ', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that R ^{12 is} not: (i) —C = C — H, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a tenth aspect of a fourth embodiment of the invention, there is provided a compound represented by Formula I-8

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

(i) R ¹⁰ represents H, F, Br, I, OH, OR ', NH ₂ , NHR', NR ' ₂ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H , or CH = CHCO ₂ R ',

where R 'represents lower alkyl, lower cycloalkyl, or C (O) (lower alkyl), or, alternatively, in the case of NR' ₂ , each R 'contains at least one C atom that binds to form a heterocycle, comprising at least two carbon atoms; and

(j) Z represents N or CR ¹² ; and

R ¹² represents H, halogen (including F, O, Br, I), OR ', NH ₂ , NHR', NR ' ₂ , NO ₂ , lower alkyl C ₁ -C ₆ , CO ₂ R', CONH ₂ , CONHR ', CONR' ₂ , CH = CHCO ₂ H, or CH = CHCO ₂ R '; with the proviso that R ^{12 is} not: (i) —C = CH, (ii) —C = CH ₂ , or (iii) —NO ₂ .

According to a fifth embodiment of the invention, there is provided a compound represented by Formula I, wherein the base is the structure represented by Formula d above, wherein R ¹¹ is H, R ¹ , R ² , R ^3a , R ^3b , R ⁴ , R ⁵ , R ⁶ , X, and Y are as defined in the Summary of the Invention.

According to a first aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-9:

Where

(a) R ¹ represents hydrogen, p-alkyl; branched alkyl; cycloalkyl; or aryl, including, but not limited to phenyl and naphthyl, where phenyl and naphthyl may optionally contain at least one of the series C _1-6 alkyl, C _2-6 alkenyl, C _2-6 alkynyl, C _{1 -6} alkoxy, F, Cl, Br, I, nitro, cyano, C _1-6 haloalkyl, -N (R ') ₂ , C _1-6 acylamino, -NHSO ₂ C _1-6 alkyl, -SO ₂ N ( Rr) ₂ , COR ^{1 ″} , and —SO ₂ C _1-6 alkyl; (R ^{1 'is} independently hydrogen or alkyl, including but not limited to C ₁ - ₂₀ alkyl, C _1-10 alkyl, or C _1-6 alkyl, R1''is-OR' or -N (R ^{1 ')} ₂ );

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a and R ^3b (i) are independently selected from hydrogen, C _1-10 alkyl, cycloalkyl, - (CH ₂ ) _c (NR ^{3 '} ) ² , C _1-6 hydroxyalkyl, -CH ₂ SH, - ( CH ₂ ) ₂ S (O) _d Me, - (CH ₂ ) ₃ NHC (= NH) NH ₂ , (1H-indol-3-yl) methyl, (1H-imidazol-4-yl) methyl, - (CH ₂ ) _e COR ³ , aryl and aryl C _1-3 alkyl, the aryl groups mentioned above may contain, as substituents, a group selected from hydrogen, C _1-10 alkyl, C _1-6 alkoxy, halogen, nitro and cyano; (ii) R ^3a and R ^{3b are} both C _1-6 alkyl; (iii) R ^3a and R ^3b together represent (CH ₂ ) _f such that a spiral ring is formed; (iv) R ^3a represents hydrogen, and R ^3b and R ² together represent (CH ₂ ) _n such that a cyclic ring is formed comprising adjacent N and C atoms (v) R ^3b is hydrogen, and R ^3a and R ² together represent (CH ₂ ) _n so that a cyclic ring is formed including neighboring atoms N and C, where c is from 1 to 6, d is from 0 to 2, e is early from 0 to 3, f is from 2 to 5, n is early from 2 to 4, and where R independently is hydrogen or C _1-6 alkyl, and R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ ); (vi) R ^3a represents H and R ^3b represents H, CH ₃ , CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ( (4'-OH) -Ph), CH ₂ SH, or lower cycloalkyl; or (viii) R ^3a represents CH ₃ , —CH ₂ CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ - indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH) —Ph), CH ₂ SH, or lower cycloalkyl, and R ^3b is H, where R ^{3 ′ is} independently hydrogen or alkyl, including, but not limited to C _1-20 alkyl, C _1-10 alkyl, or C _{1 -6} alkyl, R ^{3 ″} is —OR ′ or —N (R ^{3 ′} ) ₂ );

(d) R ⁴ represents hydrogen, C _1-10 alkyl, C _1-10 alkyl, possibly having substituents lower alkyl, alkoxy or halogen, C _1-10 haloalkyl, C _3-10 cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl , aminoacyl, di (lower alkyl) amino lower alkyl, aryl, such as phenyl, heteroaryl, such as pyridinyl, aryl containing substituents, or heteroaryl containing substituents;

(e) R ⁵ is H, lower alkyl, CN, vinyl, O- (lower alkyl), hydroxy lower alkyl, i.e. - (CH ₂ ) _p OH, where p is 1-6, including hydroxy methyl (CH ₂ OH), CH ₂ F, N ₃ , CH ₂ CN, CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , alkine (possibly containing substituents), or halogen, including F, Cl, Br, or I, with the proviso that when X is OH, the base is cytosine and R ⁶ is H, R ⁵ cannot be N ₃ and when X is OH, R ⁶ is CH ₃ or CH ₂ F, and B is a purine base, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OMe, halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, C _1-4 alkyl, C _2-4 alkenyl, C _2-4 alkynyl, vinyl, N ₃ , CN, Cl, Br, F, I, NO ₂ , OS (O) O (C _1-4 alkyl), OS (O) O (C _1-4 alkyl), OS (O) O (C _2-4 alkynyl), OS (O) O (C _2-4 alkenyl), OS _{1 -10} haloalkyl, O (aminoacyl), O (C _1-10 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _{1- 4} alkyl), S (C _2-4 alkynyl), S (C _1-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _1-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS ( O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N (C _1-4 alkyl) ₂ , or N (C _1-18 acyl) ₂ , where alkyl, alkynyl, alkenyl and vinyl, possibly contain as substituents N ₃ , CN, from one to three halogens (O, Br, F, I), NO ₂ , C (O) O (C _1-4 alkyl), C (O) O (C _{1 -4} alkyl), C (O) O (C _2-4 alkynyl), C (O) O (C _2-4 alkenyl), O (C _1-4 acyl), O (C _1-4 alkyl), O (C _2-4 alkenyl), S (C _1-4 acyl), S (C _1-4 alkyl), S (C _2-4 alkynyl), S (C _2-4 alkenyl), SO (C _1-4 acyl), SO (C _1-4 alkyl), SO (C _2-4 alkynyl), SO (C _2-4 alkenyl), SO ₂ (C _1-4 acyl), SO ₂ (C _1-4 alkyl), SO ₂ (C _2-4 alkynyl), SO ₂ (C _2-4 alkenyl), OS (O) ₂ (C _1-4 acyl), OS (O) ₂ (C _1-4 alkyl), OS (O) ₂ (C _2-4 alkenyl), NH ₂ , NH (C _1-4 alkyl), NH (C _2-4 alkenyl), NH (C _2-4 alkynyl), NH (C _1-4 acyl), N ( C _1-4 alkyl) ₂ , or N (C _1-4 acyl) ₂ ;

According to a second aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-9

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, Cl, Br, or I, with the proviso that when X is OH, R6 is CH ₃ or CH ₂ F, R ⁵ cannot be N.

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , halogen, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ (N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ ;

According to a third aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-9

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) 2, CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, CN, CH ₂ F, F, O, Br, or I; with the proviso that when X is OH, R6 is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, O, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ N ₃ , OCH ₃ , or OC (O) CH ₃ ;

According to a fourth aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-9

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

According to a fifth aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-9

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

According to a sixth aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-10:

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, or phenyl containing or not containing substituents, where at least one of the series CH ₃ , OCH ₃ , F, Cl, Br, I, nitro, cyano and CH _3-q X _q , where X represents F, O, Br, or I, and q is 1-3;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl, or R ^3a represents CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph , CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4 '-OH) -Ph), CH ₂ SH, or lower cycloalkyl, and R is H;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, N ₃ , CH ₂ CN, CH ₂ N ₃ , CH ₂ NH ₂ , CH ₂ NHCH ₃ , CH ₂ N (CH ₃ ) ₂ , halogen, including F, Cl, Br, or I, with the proviso that when X is OH, R ⁶ is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ;

(h) Y represents OH, H, CH ₃ , vinyl, N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ , NH ₂ , NHCH ₃ , NH (vinyl), NH (acetyl), NH (C (O) CH ₃ ), N (CH ₃ ) ₂ , N (C (O) CH ₃ ) ₂ ;

According to a seventh aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-10

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, CH ₂ -indol-3-yl, -CH ₂ CH ₂ SCH ₃ , CH ₂ CO ₂ H, CH ₂ C (O) NH ₂ , CH ₂ CH ₂ COOH, CH ₂ CH ₂ C (O) NH ₂ , CH ₂ CH ₂ CH ₂ CH ₂ NH ₂ , -CH ₂ CH ₂ CH ₂ NHC (NH) NH ₂ , CH ₂ -imidazol-4-yl, CH ₂ OH, CH (OH) CH ₃ , CH ₂ ((4'-OH ) -Ph), CH ₂ SH, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₃ , OCH ₃ , CH ₂ OH, CH ₂ F, halogen, including F, Cl, Br, or I, with the proviso that when X is OH, R6 is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , F, or CN;

(g) X represents H, OH, F, OCH ₃ , Cl, Br, I, NH ₂ , or N ₃ ; and

(h) Y represents OH, H, CH ₃ , vinyl, NH ₂ , N ₃ , CN, Cl, Br, F, I, OC (O) CH ₃ , OCH ₃ .

According to an eighth aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-10

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen or CH ₃ ;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ is H, CN, CH ₂ F, F, Cl, Br, or I, with the proviso that when X is OH, R ⁶ is CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, F, OCH ₃ , F, Cl, Br, I, NH ₂ or N ₃ ;

(h) Y represents H, OH, CH ₃ , F, Cl, Br, I, NH ₂ or N ₃ , OCH ₃ , or OC (O) CH ₃ ;

According to a ninth aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-10

Where

(a) R ¹ represents hydrogen, methyl, ethyl, n-propyl, iso-propyl, phenyl, p-tolyl, p-bromo-phenyl, p-chloro-phenyl, p-fluoro-phenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ ;

According to a tenth aspect of a fifth embodiment of the invention, there is provided a compound represented by formula I-10

Where

(a) R ¹ represents hydrogen, methyl, phenyl, p-bromo-phenyl, p-chloro-phenyl, p-fluorophenyl;

(b) R ² represents hydrogen;

(c) R ^3a represents H and R ^3b represents H, CH ₃ , CH (CH ₃ ) ₂ , CH ₂ CH (CH ₃ ) ₂ , CH (CH ₃ ) CH ₂ CH ₃ , CH ₂ Ph, or lower cycloalkyl;

(d) R ⁴ represents hydrogen, CH ₃ , Et, ⁱ Pr, ⁿ Pr, ⁿ Bu, 2-butyl, ^t Bu, benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, N-methyl-aziridin-2-yl, N-methyl-azetidin-3-yl, N-methyl-pyrrolidin-3-yl, N-methyl-pyrrolidin-4-yl, N-methyl-piperidin-4-yl, lower haloalkyl, or di (lower alkyl) amino lower alkyl;

(e) R ⁵ represents H, with the proviso that when X represents OH, R ⁶ represents CH ₃ or CH ₂ F, R ⁵ cannot be H;

(f) R ⁶ is H, CH ₃ , CH ₂ F, CHF ₂ , CF ₃ , or F;

(g) X represents H, OH, OCH ₃ , F, NH ₂ or N ₃ ;

(h) Y represents OH, NH ₂ , OCH ₃ , or OC (O) CH ₃ .

The following tables contain quantitative indicators corresponding to the various substituent groups, which should be considered in the light of the attached structure. These structures are the intended varieties of various aspects of the embodiments of the invention and do not imply the exhaustion of the full spectrum of the intended compound represented by the structure of formula I. However, it is contemplated that any of the cited nucleoside bases may be used in combination with any of the proposed varieties, which defines a particular combination of R ¹ , R ^2, R ^3a, R ^3b, R ^4, R ^5, R ^6, X, and Y. In each of the tables represented phosphoramidite substituent, including substituents R ^3a and R ^3b, Images us without transmitting stereochemical structure (see. the structure I-1, I-3, I-5, I-7, I-9 and above). The following compounds are intended to include compounds in which R ^{3a is} projected in the direction of the viewer, while R ^{3b is} projected in the opposite direction (see structures I-2, I-4, I-6, I-8, and I- 10). Moreover, it is assumed that the following compounds also include compounds in which R ^{3a is} projected in the opposite direction from the viewer, and R ^{3b is} projected in the direction of the viewer. Not being exhaustive, however, it is contemplated that preferred compounds are those in which R ^{3a is} projected in the direction of the viewer, while R ^{3b is} projected in the opposite direction, in the S configuration in which natural L-amino acids are represented. In addition, the inventors recognize that the phosphorus atom of the phosphoramidate moiety is another source of chirality. Although the structures presented below do not display chirality in phosphorus, the inventors acknowledge that structures are likely where in the stepped (or zigzag) linear structure, the oxo substituent is projected in the direction of the viewer, while the OR ¹ substituent is projected in the opposite direction from the viewer , and vice versa, i.e. correspond to Cahn-Ingold-Prelog R and S stereochemical designations. Thus, the structures presented below include all possible stereochemical configurations possible for phosphorus.

Table II-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-1-1 CH ₃ N N N CH ₃ N CH ₃ IT it n n NH ₂ II-1-2 CH ₃ N N CH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n NH ₂ II-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n NH ₂ II-1-5 CH ₃ N N CH ₂ Ph CH ₃ N CH ₃ it it n n NH ₂ II-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N CH ₃ it it n n NH ₂ II-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-1-8 CH ₃ * n * CH ₃ N CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-2-1 Et H H H CH ₃ N CH ₃ it it n n NH ₂ II-2-2 Et H H CH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n NH ₂ II-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ Chj N CH ₃ it it n n NH ₂ II-2-5 Et H H CH ₂ Ph CH ₃ N CH ₃ it it n n NH ₂ II-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N CH ₃ it it n n NH ₂ II-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ it it n n NH ₂

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-2-8 Et * N * CH ₃ N CH ₃ it IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-3-1 ⁱ Pr N N N CH ₃ N CH ₃ IT it n n NH ₂ II-3-2 ⁱ Pr N N CH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ n CH ₃ it it n n NH ₂ II-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ it it n n NH ₂ II-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ n CH ₃ it it n n NH ₂ II-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ n CH ₃ it it n n NH ₂ II-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ it it n n NH ₂ II-3-8 ⁱ Pr * n * CH ₃ n CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-4-1 ⁱ wu N N H CH ₃ N CH ₃ it it n n NH ₂ II-4-2 ⁱ wu n N CH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-4-3 ⁱ wu n n CH (CH ₃ ) 2 CH ₃ N CH ₃ it it n n NH ₂ II-4-4 ⁱ wu N N CH ₂ CH (CH ₃ ) 2 CH ₃ N CH ₃ it it n n NH ₂ II-4-5 ⁱ wu n N CH ₂ Ph CH ₃ N CH ₃ it it n n NH ₂ II-4-6 ⁱ wu n N CH ₂ -indol-3-yl CH ₃ N CH ₃ it it n n NH ₂ II-4-7 ⁱ wu n N CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-4-8 ⁱ wu * N CH ₃ N CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-5-1 Ph H H H CH ₃ N CH ₃ it it n n NH ₂ II-5-2 Ph H H CH ₃ CH ₃ N CH ₃ it it n n NH ₂ II-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n NH ₂ II-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n NH ₂ II-5-5 Ph H H CH ₂ Ph CH ₃ N CH ₃ it it n n NH ₂ II-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ it it n n NH ₂

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-5-7 Ph N N CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ OH IT N N NH ₂ II-5-8 Ph * N * CH ₃ N CH ₃ OH IT N H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-6-1 p-me-ph H H H CH ₃ N CH ₃ IT IT N N NH ₂ II-6-2 p-me-ph H H CH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-6-5 p-me-ph H H CH ₂ Ph CH ₃ N CH ₃ IT IT N N NH ₂ II-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ IT IT N N NH ₂ II-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-6-8 p-me-ph * H * CH ₃ N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-7-1 p-f-ph H H H CH ₃ N CH ₃ IT IT N N NH ₂ II-7-2 p-f-ph H H CH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-7-6 p-f-ph H H CH ₂ Ph CH ₃ N CH ₃ IT IT N N NH ₂ II-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ IT IT N N NH ₂ II-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-7-20 p-f-ph * H * CH ₃ N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-8-1 p-Cl-Ph H H H CH ₃ N CH ₃ IT IT N N NH ₂ II-8-2 p-Cl-Ph H H CH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N CH ₃ IT IT N N NH ₂

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ IT IT N N NH ₂ II-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-8-8 p-Cl-Ph * H * CH ₃ n CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring .. Table II-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-9-1 r-br-ph H H H CH ₃ n CH ₃ IT IT N N NH ₂ II-9-2 p-Br-Ph H H CH ₃ CH ₃ n CH ₃ IT IT N N NH ₂ II-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ IT IT N N NH ₂ II-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ IT IT N N NH ₂ II-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n CH ₃ IT IT N N NH ₂ II-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ IT IT N N NH ₂ II-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ IT IT N N NH ₂ II-9-20 p-Br-Ph * H * CH ₃ n CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-10. No. R ¹ R ² R ^3a R ^3b R ⁵ R ⁶ R ⁷ X Y R ⁷ R ⁸ R ⁹ II-10-1 p-1-ph N H N CH ₃ N CH ₃ IT IT N N NH ₂ II-10-2 p-1-ph N n CH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-10-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT IT N N NH ₂ II-10-5 p-1-ph N N CH ₂ Ph CH ₃ N CH ₃ IT IT N N NH ₂ II-10-6 p-1-ph N N CH ₂ -indol-3-yl CH ₃ N CH ₃ IT IT N N NH ₂ II-10-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ IT IT N N NH ₂ II-10-8 p-1-ph * N * CH ₃ N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-11-1 CH ₃ H N N Et H CH ₃ OH IT N N NH ₂ II-11-2 CH ₃ H N CH ₃ Et H CH ₃ IT IT N N NH ₂ II-11-3 CH ₃ H n CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-11-4 CH ₃ H n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ OH IT N N NH ₂

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-11-5 CH ₃ H H CH ₂ Ph Et n CH ₃ IT IT N N NH ₂ II-11-6 CH ₃ H H CH ₂ -indol-3-yl Et n CH ₃ IT IT N N NH ₂ II-11-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ Et n CH ₃ IT IT N N NH ₂ II-11-8 CH ₃ * H * Et n CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-12-1 Et H H H Et N CH ₃ IT IT N N NH ₂ II-12-2 Et H H CH ₃ Et N CH ₃ IT IT N N NH ₂ II-12-3 Et H H CH (CH ₃ ) ₂ Et N CH ₃ IT IT N N NH ₂ II-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et N CH ₃ IT IT N N NH ₂ II-12-5 Et H H CH ₂ Ph Et N CH ₃ IT IT N N NH ₂ II-12-6 Et H H CH ₂ -indol-3-yl Et N CH ₃ IT IT N N NH ₂ II-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et N CH ₃ IT IT N N NH ₂ II-12-8 Et * N * Et N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-13-1 ⁱ Pr H H H Et N CH ₃ IT IT N N NH ₂ II-13-2 ⁱ Pr H H CH ₃ Et N CH ₃ IT IT N N NH ₂ II-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et N CH ₃ IT IT N N NH ₂ II-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et N CH ₃ IT IT N N NH ₂ II-13-5 ⁱ Pr H H CH ₂ Ph Et N CH ₃ IT IT N N NH ₂ II-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et N CH ₃ IT IT N N NH ₂ II-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et N CH ₃ IT IT N N NH ₂ II-13-8 ⁱ Pr * N * Et N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-14-1 ^t Bu H H H Et N CH ₃ IT IT N N NH ₂ II-14-2 ^t Bu H H CH ₃ Et N CH ₃ IT IT N N NH ₂

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-14-3 ‘Wu H H CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-14-4 ‘Wu H H CH ₂ CH (CH ₃ ) 2 Et H CH ₃ IT IT N N NH ₂ II-14-5 ‘Wu H H CH ₂ Ph Et H CH ₃ IT IT N N NH ₂ II-14-6 ‘Wu H H CH ₂ -indol-3-yl Et H CH ₃ IT IT N N NH ₂ II-14-7 ‘Wu H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT N N NH ₂ II-14-8 ‘Wu * H * Et H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-15-1 Ph H H H Et H CH ₃ IT IT N N NH ₂ II-15-2 Ph H H CH ₃ Et H CH ₃ IT IT N N NH ₂ II-15-3 Ph H H CH (CH ₃ ) 2 Et H CH ₃ IT IT N N NH ₂ II-15-4 Ph H H CH ₂ CH (CH ₃ ) 2 Et H CH ₃ IT IT N N NH ₂ II-15-5 Ph H H CH ₂ Ph Et H CH ₃ IT IT N N NH ₂ II-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ IT IT N N NH ₂ II-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT N N NH ₂ II-15-8 Ph * H * Et H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-16-1 p-me-ph H H N Et N CH ₃ IT IT H H NH ₂ II-16-2 p-me-ph H H CH ₃ Et H CH ₃ IT IT H H NH ₂ II-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ IT IT H H NH ₂ II-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ IT IT H H NH ₂ II-16-5 p-me-ph H H CH ₂ Ph Et H CH ₃ IT IT H H NH ₂ II-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ IT IT H H NH ₂ II-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT H H NH ₂ II-16-8 p-me-ph * H * Et H CH ₃ IT IT H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-17-1 p-f-ph H H H Et H CH ₃ IT IT N N NH ₂ II-17-2 p-f-ph H H CH ₃ Et H CH ₃ IT IT N N NH ₂ II-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ IT IT N N NH ₂ II-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ IT IT N N NH ₂ II-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT N N NH ₂ II-17-8 p-f-ph * H * Et H CH ₃ IT IT N N NH ₂ * R ² and RR ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-18. No. R R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-18-1 p-Cl-Ph H H H Et H CH ₃ IT IT N N NH ₂ II-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ IT IT N N NH ₂ II-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-8-5 p-Cl-Ph H H CH ₂ Ph Et H CH ₃ IT IT N N NH ₂ II-18-6 p-Cl-Ph H H CHg-indol-3-yl Et H CH ₃ IT IT N N NH ₂ II-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT N N NH ₂ II-18-8 p-Cl-Ph * H * Et H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) s to form a five-membered ring. Table II-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-19-1 p-Br-Ph H H H Et H CH ₃ IT IT N N NH ₂ II-19-2 p-Br-Ph H H CH ₃ Et H CH ₃ IT IT N N NH ₂ II-19-3 r-vg-ph H H CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ IT IT N N NH ₂ II-19-5 p-Br-Ph H H CH ₂ Ph Et H CH ₃ IT IT N N NH ₂ II-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H CH ₃ IT IT N N NH ₂ II-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT N N NH ₂ II-19-8 p-Br-Ph * H * Et H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-20-1 p-1-ph N N N Et H CH ₃ IT IT N N NH ₂ II-20-2 p-1-ph N N CH ₃ Et H CH ₃ IT IT N N NH ₂ II-20-3 p-1-ph N N CH (CH ₃ ) 2 Et H CH ₃ IT IT N N NH ₂ II-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) 2 Et H CH ₃ IT IT N N NH ₂ II-20-5 p-1-ph N N CH ₂ Ph Et H CH ₃ IT IT N N NH ₂ II-20-6 p-1-ph N N CH ₂ -indol-3-yl Et H CH ₃ IT IT N N NH ₂ II-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ IT IT N N NH ₂ II-20-8 p-1-ph * n * Et H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-21. No. R R R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-21-1 CH ₃ N N n ⁱ Pr N CH ₃ IT IT N N NH ₂ II-21-2 CH ₃ N N CH ₃ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ IT IT N N NH ₂ II-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ IT IT N N NH ₂ II-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr n CH ₃ IT IT N N NH ₂ II-21-6 CH ₃ N N CH ₂ -indol-3-yl ⁱ Pr n CH ₃ IT IT N N NH ₂ II-21-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ IT IT N N NH ₂ II-21-8 CH ₃ * N * ⁱ Pr n CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) 3 to form a five-membered ring. Table II-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-22-1 Et H H H ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-22-8 Et * H * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-23-1 ⁱ Pr N N N ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-2 ⁱ Pr N N CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-23-8 ⁱ Pr * N * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-24-1 ^t bu N N n ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-2 ^t bu N N CH ₃ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-3 ^t bu N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-5 ^t bu N N CH ₂ Ph ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-6 ^t bu N N CH ₂ -indol-3-yl ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-7 ^t bu N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-24-8 ^t bu * N * ⁱ Pr N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R5 R ⁶ X Y R ⁷ R ⁸ R ⁹ II-25-1 Ph H H H ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-25-8 Ph * H * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-26-1 p-me-ph H H H ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-S p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-26-8 p-me-ph * H * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-27-1 p-f-ph H H H ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-27-8 p-f-ph * H * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-28-1 p-Cl-Ph H H H ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-28-8 p-Cl-Ph * H * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ IT IT N N NH ₂ II-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-30-1 p-1-ph N N N ⁱ Pr N CH ₃ IT IT N N NH ₂ II-30-2 p-1-ph N N CH ₃ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-30-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-30-5 p-1-ph N N CH ₂ Ph ⁱ Pr N CH ₃ IT IT N N NH ₂ II-30-6 p-1-ph N N CH ₂ -indol-3-yl ⁱ Pr N CH ₃ IT IT N N NH ₂ : II-30-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ IT IT N N NH ₂ II-30-8 p-1-ph * N * ⁱ Pr N CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-31-1 CH ₃ N N n ⁿ Bu H CH ₃ IT IT N N NH ₂ II-31-2 CH ₃ N N CH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ P-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H CH ₃ IT IT N N NH ₂ II-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT IT N N NH ₂ II-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-31-8 CH ₃ * N * ⁿ Bu H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-32-1 Et H H H ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-32-8 Et * H * ⁿ Bu H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-33-1 ⁱ Pr H H H ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-33-8 ⁱ Pr * H * ⁿ Bu H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-34-1 ^t Bu H H H ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-2 ^t Bu H H CH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-34-8 ^t Bu * H * ⁿ Bu H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-35-1 Ph H H H ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-35-8 Ph * H * ⁿ Bu H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-36-1 p-me-ph H H H ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ IT IT N N NH ₂ II-36-8 p-me-ph * H ⁿ Bu H CH ₃ IT IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-37-1 p-f-ph H H H ⁿ Bu H CH ₃ IT IT n n NH ₂ II-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ IT it n n NH ₂ II-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n NH ₂ II-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n NH ₂ II-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n NH ₂ II-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n NH ₂ II-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n NH ₂ II-37-8 p-f-ph * H * ⁿ Bu H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ it it n n NH ₂ H-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ it it n n NH2 II-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n NH ₂ II-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n NH ₂ II-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n NH ₂ II-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n NH ₂ I-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n NH ₂ II-38-8 p-Cl-Ph * H * ⁿ Bu H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ it it n n NH ₂ II-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ IT it n n NH ₂ H-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n NH ₂ II-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n NH ₂ II-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n NH ₂ II-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n NH ₂ II-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n NH ₂ II-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-40-1 p-1-ph N n n ⁿ Bu H CH ₃ IT IT n n NH ₂ II-40-2 p-1-ph N n CH ₃ ⁿ Bu H CH ₃ IT IT n n NH ₂ II-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n NH ₂ II-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n NH ₂ II-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H CH ₃ IT it n n NH ₂ II-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT it n n NH ₂ II-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n NH ₂ II-40-8 p-1-ph * n * ⁿ Bu H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-41-1 CH ₃ N N H Bz H CH ₃ it it n n NH ₂ II-41-2 CH ₃ N N CH ₃ Bz H CH ₃ it it n n NH ₂ II-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-41-5 CH ₃ N n CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-41-8 CH ₃ * n * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-42-1 Et H H H Bz H CH ₃ it it n n NH ₂ II-42-2 Et H H CH ₃ Bz H CH ₃ it it n n NH ₂ II-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-42-5 Et H H CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-42-8 Et * H * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-43-1 ⁱ Pr N n n Bz H CH ₃ IT it n n NH ₂ II-43-2 ⁱ Pr N n CH ₃ Bz H CH ₃ IT it n n NH ₂ II-43-3 ⁱ Pr n n CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n NH ₂ P-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-43-5 ⁱ Pr n n CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-43-8 ⁱ Pr * n * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-44-1 ^t bu N N n Bz H CH ₃ it it n n NH ₂ II-44-2 ^t bu N N CH ₃ Bz H CH ₃ it it n n NH ₂ II-44-3 ^t bu N n CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-44-5 ^t bu N n CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-44-8 ^t bu * n * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-45-1 Ph H H H Bz H CH ₃ IT IT n n NH ₂ II-45-2 Ph H H CH ₃ Bz H CH ₃ IT it n n NH ₂ II-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n NH ₂ II-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n NH ₂ II-45-5 Ph H H CH ₂ Ph Bz H CH ₃ IT it n n NH ₂ II-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ IT it n n NH ₂ II-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ IT it n n NH ₂ II-45-8 Ph H * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-46-1 p-me-ph H H H Bz H CH ₃ OH OH n n NH ₂ II-46-2 p-me-ph H H CH ₃ Bz H CH ₃ OH OH n n NH ₂ II-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ OH OH n n NH ₂ II-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ OH OH n n NH ₂ II-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ OH OH n n NH ₂ II-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ OH OH n n NH ₂ II-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ OH OH n n NH ₂ II-46-8 p-me-ph * H * Bz H CH ₃ OH OH n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ I-47-1 p-f-ph H H H Bz H CH ₃ it it n n NH ₂ II-47-2 p-f-ph H H CH ₃ Bz H CH ₃ it it n n NH ₂ II-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ P-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ P-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-47-8 p-f-ph * H * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table II-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-48-1 p-Cl-Ph H H H Bz H CH ₃ it it n n NH ₂ II-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ it it n n NH ₂ II-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-48-8 p-Cl-Ph * H * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) s to form a five-membered ring. Table II-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-49-1 p-Br-Ph H H H Bz H CH ₃ it it n n NH ₂ II-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ it it n n NH ₂ II-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-49-8 p-Br-Ph * H * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table II-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ II-50-1 p-1-ph N n H Bz H CH ₃ IT it n n NH ₂ II-50-2 p-1-ph N n CH ₃ Bz H CH ₃ it it n n NH ₂ I-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ I-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n NH ₂ II-50-5 p-1-ph N n CH ₂ Ph Bz H CH ₃ it it n n NH ₂ II-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H CH ₃ it it n n NH ₂ II-50-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n NH ₂ II-50-8 p-1-ph * n * Bz H CH ₃ it it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-1-1 CH ₃ N n n CH ₃ N CH ₃ F IT N N NH ₂ III-1-2 CH ₃ N n CH ₃ CH ₃ N CH ₃ F IT N N NH ₂ III-1-3 CH ₃ n n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N NH ₂ III-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N NH ₂ III-1-5 CH ₃ n n CH ₂ Ph CH ₃ N CH ₃ F IT N N NH ₂ III-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT N N NH ₂ III-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT N N NH ₂ III-1-8 CH ₃ * n * CH ₃ n CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-2-1 Et H H H CH ₃ n CH ₃ F IT N n NH ₂ III-2-2 Et H H CH ₃ CH ₃ n CH ₃ F IT N n NH ₂ III-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n NH ₂ III-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n NH ₂ III-2-5 Et H H CH ₂ Ph CH ₃ n CH ₃ F IT n n NH ₂ III-2-6 Et H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT n n NH ₂ III-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT n n NH ₂ III-2-8 Et * H CH ₃ n CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-3-1 ⁱ Pr N N N CH ₃ n CH ₃ F IT N N NH ₂ III-3-2 ⁱ Pr N N CH ₃ CH ₃ n CH ₃ F IT N N NH ₂ III-3-3 ⁱ Pr n N CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT N N NH ₂ III-3-4 ⁱ Pr n N CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT N N NH ₂ III-3-5 ⁱ Pr n N CH ₂ Ph CH ₃ n CH ₃ F IT N N NH ₂ III-3-6 ⁱ Pr n n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT N N NH ₂ III-3-7 ⁱ Pr n N CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT N N NH ₂ III-3-8 ⁱ Pr * N * CH ₃ n CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring Table III-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-4-1 ^t bu N n n CH ₃ N CH ₃ F IT N N NH ₂ III-4-2 ^t bu N n CH ₃ CH ₃ N CH ₃ F IT N N NH ₂ III-4-3 ^t bu n n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N NH ₂ III-4-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N NH ₂ III-4-5 ^t bu n n CH ₂ Ph CH ₃ N CH ₃ F IT N N NH ₂ III-4-6 ^t bu n n CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT N N NH ₂ III-4-7 ^t bu n n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT N N NH ₂ III-4-8 ^t bu * n * CH ₃ N CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-5-1 Ph H H H CH ₃ n CH ₃ F IT n n NH ₂ III-5-2 Ph H H CH ₃ CH ₃ n CH ₃ F IT n n NH ₂ III-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F it n n NH ₂ III-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F it n n NH ₂ III-5-5 Ph H H CH ₂ Ph CH ₃ n CH ₃ F it n n NH ₂ III-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F it n n NH ₂ III-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F it n n NH ₂ III-5-8 Ph * H * CH ₃ n CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-6-1 p-me-ph H H H CH ₃ N CH ₃ F IT N N NH ₂ III-6-2 p-me-ph H H CH ₃ CH ₃ N CH ₃ F IT N N NH ₂ III-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n N NH ₂ III-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n N NH ₂ III-6-5 p-me-ph H H CH ₂ Ph CH ₃ N CH ₃ F IT n n NH ₂ III-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT n n NH ₂ III-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT n n NH ₂ III-6-8 p-me-ph * H * CH ₃ N CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-7-1 p-f-ph H H H CH ₃ N CH ₃ F IT N N NH ₂ III-7-2 p-f-ph H H CH ₃ CH ₃ N CH ₃ F IT N N NH ₂ III-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N NH ₂ III-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N NH ₂ III-7-6 p-f-ph H H CH ₂ Ph CH ₃ N CH ₃ F IT N N NH ₂ III-7-7 p-f-ph H H CH ₂ -indole-3 -yl CH ₃ N CH ₃ F IT n N NH ₂ III-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT n n NH ₂ III-7-20 p-f-ph * H * CH ₃ N CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-8-1 p-Cl-Ph H H H CH ₃ H CH ₃ F IT N n NH ₂ III-8-2 p-Cl-Ph H H CH ₃ CH ₃ H CH ₃ F IT N n NH ₂ III-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F IT n n NH ₂ III-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F IT n n NH ₂ III-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ H CH ₃ F IT n n NH ₂ III-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F IT n n NH ₂ III-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F IT n n NH ₂ III-8-8 p-Cl-Ph * H * CH ₃ H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-9-1 p-Br-Ph H H H CH ₃ N CH ₃ F IT N N NH ₂ III-9-2 p-Br-Ph H H CH ₃ CH ₃ n CH ₃ F IT N N NH ₂ III-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT N N NH ₂ III-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT N n NH ₂ III-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n CH ₃ F IT N n NH ₂ III-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT N n NH ₂ III-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT N n NH ₂ III-9-20 p-Br-Ph * H * CH ₃ n CH ₃ F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-10-1 p-1-ph N N n CH ₃ N CH ₃ F IT n n NH ₂ III-10-2 p-1-ph N n CH ₃ CH ₃ N CH ₃ F IT n n NH ₂ III-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n NH ₂ III-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n NH ₂ III-10-5 p-1-ph N n CH ₂ Ph CH ₃ n CH ₃ F IT n n NH ₂ III-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT n n NH ₂ III-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F it n n NH ₂ III-10-8 p-1-ph * n * CH ₃ n CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-11-1 CH ₃ N N n Et H CH ₃ F IT N n NH ₂ III-11-2 CH ₃ N N CH ₃ Et H CH ₃ F IT n n NH ₂ III-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H CH ₃ F IT n n NH ₂ III-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n n NH ₂ III-11-5 CH ₃ N n CH ₂ Ph Et H CH ₃ F IT n n NH ₂ III-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H CH ₃ F IT n n NH ₂ III-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n NH ₂ III-11-8 CH ₃ * n * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-12-1 Et H H H Et H CH ₃ F IT N N NH ₂ III-12-2 Et H H CH ₃ Et H CH ₃ F IT N N NH ₂ III-12-3 Et H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N N NH ₂ III-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N N NH ₂ III-12-5 Et H H CH ₂ Ph Et H CH ₃ F IT N N NH ₂ III-12-6 Et H H CH ₂ -indol-3-yl Et H CH ₃ F IT N N NH ₂ III-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N N NH ₂ III-12-8 Et * H Et H CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-13-1 ⁱ Pr N N n Et H CH ₃ F IT N N NH ₂ III-13-2 ⁱ Pr N N CH ₃ Et H CH ₃ F IT N N NH ₂ III-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H CH ₃ F IT N N NH ₂ III-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N N NH ₂ III-13-5 ⁱ Pr N n CH ₂ Ph Et H CH ₃ F IT N N NH ₂ III-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H CH ₃ F IT N N NH ₂ III-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N N NH ₂ III-13-8 ⁱ Pr * n * Et H CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-14-1 ^t bu N n H Et H CH ₃ F IT N n NH ₂ III-14-2 ^t bu n n CH ₃ Et H CH ₃ F IT N n NH ₂ III-14-3 ^t bu n n CH (CH ₃ ) ₂ Et H CH ₃ F IT N n NH ₂ III-14-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n NH ₂ III-14-5 ^t bu n n CH ₂ Ph Et H CH ₃ F IT N n NH ₂ III-14-6 ^t bu n n CH ₂ -indol-3-yl Et H CH ₃ F IT N n NH ₂ III-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N n NH ₂ III-14-8 ^t bu n * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-15-1 Ph H H H Et H CH ₃ F IT N n NH ₂ III-15-2 Ph H H CH ₃ Et H CH ₃ F IT N n NH ₂ III-15-3 Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N n NH ₂ III-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n NH ₂ III-15-5 Ph H H CH ₂ Ph Et H CH ₃ F IT n n NH ₂ III-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n NH ₂ III-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n NH ₂ III-15-8 Ph * H * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-16-1 p-me-ph H H H Et H CH ₃ F IT N n NH ₂ III-16-2 p-me-ph H H CH ₃ Et H CH ₃ F IT N n NH ₂ III-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N n NH ₂ III-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n NH ₂ III-6-5 p-me-ph H H CH ₂ Ph Et H CH ₃ F IT N n NH ₂ III-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT N n NH ₂ III-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N n NH ₂ III-16-8 p-me-ph * H * Et H CH ₃ F IT n n NH ₂

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-17-1 p-f-ph H H H Et H CH ₃ F IT N n NH ₂ III-17-2 p-f-ph H H CH ₃ Et H CH ₃ F IT N n NH ₂ III-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT n n NH ₂ III-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n n NH ₂ III-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ F IT n n NH ₂ III-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n NH ₂ III-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n NH ₂ III-17-8 p-f-ph H * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-18-1 p-Cl-Ph H H H Et H CH ₃ F IT N N NH ₂ III-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ F IT N N NH ₂ III-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT n N NH ₂ III-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n N NH ₂ III-18-5 p-Cl-Ph H H CH ₂ Ph Et H CH ₃ F IT n n NH ₂ III-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n NH ₂ III-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n NH ₂ III-18-8 p-Cl-Ph * H * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-19-1 p-Br-Ph H H H Et H CH ₃ F IT N N NH ₂ III-19-2 p-Br-Ph H H CH ₃ Et H CH ₃ F IT N N NH ₂ III-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT n N NH ₂ III-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n N NH ₂ III-19-5 p-Br-Ph H H CH ₂ Ph Et H CH ₃ F IT n n NH ₂ III-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n NH ₂ III-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n NH ₂ III-19-8 p-Br-Ph * H * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-20-1 p-1-ph H N H Et H CH ₃ F IT N N NH ₂ III-20-2 p-1-ph N N CH ₃ Et H CH ₃ F IT N N NH ₂ III-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et H CH ₃ F IT n N NH ₂ III-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n n NH ₂ III-20-5 p-1-ph N n CH ₂ Ph Et H CH ₃ F IT n n NH ₂ III-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H CH ₃ F IT n n NH ₂ III-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n NH ₂ III-20-8 p-1-ph * n * Et H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IH-21-1 CH ₃ N n n ⁱ Pr N CH ₃ F IT N N NH ₂ III-21-2 CH ₃ N n CH ₃ ⁱ Pr n CH ₃ F IT N N NH ₂ III-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT N n NH ₂ III-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ n CH ₃ F IT N n NH ₂ III-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr n CH ₃ F IT N n NH ₂ III-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT N n NH ₂ III-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT N n NH ₂ III-21-8 CH ₃ * n * ⁱ Pr n CH ₃ F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-22-1 Et H H H ⁱ Pr H CH ₃ F IT N N NH ₂ III-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ F IT N N NH ₂ III-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n NH ₂ III-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n NH ₂ III-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ F IT N n NH ₂ III-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT N n NH ₂ III-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT N n NH ₂ III-22-8 Et * H * ⁱ Pr H CH ₃ F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-23-1 ⁱ Pr N N H ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT N N NH ₂ III-23-8 ⁱ Pr * n * ⁱ Pr N CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-24-1 ^t bu N n H ⁱ Pr N CH ₃ F IT N N NH ₂ III-24-2 ^t bu N n CH ₃ ⁱ Pr N CH ₃ F IT N N NH ₂ III-24-3 ^t bu n n CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N NH ₂ III-24-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N NH ₂ III-24-5 ^t bu n n CH ₂ Ph ⁱ Pr n CH ₃ F IT N N NH ₂ III-24-6 ^t bu n n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT N N NH ₂ III-24-7 ^t bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT N N NH ₂ III-24-8 ^t bu n * ⁱ Pr n CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table 111-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-25-1 Ph H H H ⁱ Pr H CH ₃ F IT N n NH ₂ III-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ F IT N n NH ₂ III-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n NH ₂ III-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n NH ₂ III-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT n n NH ₂ IH-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n n NH ₂ III-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n NH ₂ III-25-8 Ph * H * ⁱ Pr H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-26-1 p-me-ph H H H ⁱ Pr H CH ₃ F IT N n NH ₂ III-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ F IT N n NH ₂ III-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n NH ₂ III-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n NH ₂ III-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT n n NH ₂ III-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n n NH ₂ III-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n NH ₂ III-26-8 p-me-ph * H * ⁱ Pr H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-27-1 p-f-ph H H H ⁱ Pr H CH ₃ F IT n n NH ₂ III-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ F IT n n NH ₂ III-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F it n n NH _2. • ' III-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F it n n NH ₂ III-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F it n n NH ₂ III-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F it n n NH ₂ * III-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F it n n NH ₂ III-27-8 p-f-ph * H ⁱ Pr H CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table 111-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-28-1 p-Cl-Ph H H H ⁱ Pr H CH ₃ F IT N n NH ₂ IH-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H CH ₃ F IT N n NH ₂ III-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Tr H CH ₃ F IT n n NH ₂ III-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n NH ₂ III-28-5 p-Cl-Ph H H CH ₂ Ph • Pr H CH ₃ F IT n n NH ₂ III-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n n NH ₂ III-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n NH ₂ III-28-8 p-Cl-Ph * H * ⁱ Pr H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ F IT n n NH ₂ III-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ F IT n n NH ₂ III-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n NH ₂ III-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F it n n NH ₂ III-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F it n n NH ₂ III-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F it n n NH ₂ III-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F it n n NH ₂ III-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-30-1 p-1-ph N N n ⁱ Pr N CH ₃ F IT N N NH ₂ III-30-2 p-1-ph N n CH ₃ ⁱ Pr N CH ₃ F IT N N NH ₂ III-30-3 p-1-ph N n CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT N N NH ₂ III-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT N N NH ₂ III-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr n CH ₃ F IT N N NH ₂ III-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT N N NH ₂ III-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT N N NH ₂ III-30-8 p-1-ph * n ⁱ Pr n CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-31-1 CH ₃ N N n ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-2 CH ₃ N N CH ₃ ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N N NH ₂ III-31-8 CH ₃ * n * ⁿ Bu H CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-32-1 Et H H H ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N n NH ₂ III-32-8 Et * H * ⁿ Bu H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-33-1 ⁱ Pr N N n ⁿ Bu H CH ₃ F IT n N NH ₂ III-33-2 ⁱ Pr N N CH ₃ ⁿ Bu H CH ₃ F IT n n NH ₂ III-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT n n NH ₂ III-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT n n NH ₂ III-33-5 ⁱ Pr N n CH ₂ Ph ⁿ Bu H CH ₃ F it n n NH ₂ III-33-6 ⁱ Pr N n CH ₂ -indole-3 -yl ⁿ Bu H CH ₃ F it n n NH ₂ III-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F it n n NH ₂ III-33-8 ⁱ Pr * n * ⁿ Bu H CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-34-1 ^t bu N N N ⁿ b N CH ₃ F IT N N NH ₂ III-34-2 ^t bu N N CH ₃ ⁿ b N CH ₃ F IT N N NH ₂ III-34-3 ^t bu n N CH (CH ₃ ) ₂ ⁿ b n CH ₃ F IT n N NH ₂ III-34-4 ^t bu n N CH ₂ CH (CH ₃ ) ₂ ⁿ b n CH ₃ F IT n N NH ₂ III-34-5 ^t bu n N CH ₂ Ph ⁿ b n CH ₃ F IT n n NH ₂ III-34-6 ^t bu n N CH ₂ -indol-3-yl ⁿ b n CH ₃ F IT n n NH ₂ III-34-7 ^t bu n N CH ₂ CH ₂ SCH ₃ ⁿ b n CH ₃ F IT n n NH ₂ III-34-8 ^t bu * N * ⁿ b n CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-35-1 Ph H H H ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N N NH ₂ III-35-8 Ph * H * ⁿ Bu H CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-36-1 p-me-ph H H H ⁿ Bu H CH ₃ F IT N n NH ₂ III-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ F IT N n NH ₂ III-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT n n NH ₂ III-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT n n NH ₂ III-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT n n NH ₂ III-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT n n NH ₂ III-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT n n NH ₂ III-36-8 p-me-ph * H * ⁿ Bu H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-37-1 p-f-ph H H H ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-6 p-f-ph H H CH ₂ -INDOL-3-IL ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N N NH ₂ III-37-8 p-f-ph * H * ⁿ Bu H CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F OH H H NH ₂ III-38-8 p-Cl-Ph * H * ⁿ Bu H CH ₃ F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F OH H H NH ₂ III-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-40-1 p-1-ph N n n ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-2 p-1-ph N n sun ₃ ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F OH H H NH ₂ III-40-8 p-1-ph * n * ⁿ Bu H CH ₃ F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-41-1 CH ₃ N n n Bz H CH ₃ F IT N N NH ₂ III-41-2 CH ₃ N n CH ₃ Bz H CH ₃ F IT N N NH ₂ III-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N NH ₂ III-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N NH ₂ III-41-5 CH ₃ N n CH ₂ Ph Bz H CH ₃ F IT n n NH ₂ III-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz H CH ₃ F IT n n NH ₂ III-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n NH ₂ III-41-8 CH ₃ * n * Bz H CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-42-1 Et H H H Bz H CH ₃ F IT N N NH ₂ III-42-2 Et H H CH ₃ Bz H CH ₃ F IT N N NH ₂ III-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT n N NH ₂ III-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n N NH ₂ III-42-5 Et H H CH ₂ Ph Bz H CH ₃ F IT n n NH ₂ III-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ F IT n n NH ₂ III-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n NH ₂ III-42-8 Et * H Bz H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-43-1 ⁱ Pr N n n Bz H CH ₃ F IT N N NH ₂ III-43-2 ⁱ Pr N n CH ₃ Bz H CH ₃ F IT N N NH ₂ III-43-3 ⁱ Pr n n CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-43-5 ⁱ Pr n n CH ₂ Ph Bz H CH ₃ F IT N n NH ₂ III-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz H CH ₃ F IT N n NH ₂ IH-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n NH ₂ III-43-8 ⁱ Pr * n * Bz H CH ₃ F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-44-1 ^t bu N N H Bz H CH ₃ F IT N N NH ₂ III-44-2 ^t bu N n CH ₃ Bz H CH ₃ F IT N N NH ₂ III-44-3 ^t bu N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N NH ₂ III-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-44-5 ^t bu N n CH ₂ Ph Bz H CH ₃ F IT N n NH ₂ III-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H CH ₃ F IT N n NH ₂ III-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n NH ₂ III-44-8 ^t bu * n * Bz H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-45-1 Ph H H H Bz H CH ₃ F IT N n NH ₂ III-45-2 Ph H H CH ₃ Bz H CH ₃ F IT N n NH ₂ III-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-45-5 Ph H H CH ₂ Ph Bz H CH ₃ F IT N n NH ₂ III-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT n n NH ₂ III-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n NH ₂ III-45-8 Ph * H * Bz H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-46-1 p-me-ph H H H Bz H CH ₃ F IT N N NH ₂ III-46-2 p-me-ph H H CH ₃ Bz H CH ₃ F IT N N NH ₂ III-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N NH ₂ III-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N NH ₂ III-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ F IT N N NH ₂ IH-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT N N NH ₂ III-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N N NH ₂ III-46-8 p-me-ph * H * Bz H CH ₃ F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-47-1 p-f-ph H H H Bz H CH ₃ F IT N n NH ₂ III-47-2 p-f-ph H H CH ₃ Bz H CH ₃ F IT N n NH ₂ III-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT n n NH ₂ III-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n n NH ₂ III-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ F IT n n NH ₂ III-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT n n NH ₂ III-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n NH ₂ III-47-8 p-f-ph * H * Bz H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table III-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-48-1 p-Cl-Ph H H H Bz H CH ₃ F IT N n NH ₂ III-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ F IT N n NH ₂ III-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n NH ₂ III-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ F IT N n NH ₂ III-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT N n NH ₂ III-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n NH ₂ III-48-8 p-Cl-Ph * H * Bz H CH ₃ F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring Table III-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-49-1 p-Br-Ph H H H Bz H CH ₃ F IT N N NH ₂ III-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ F IT N N NH ₂ III-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT n N NH ₂ III-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n N NH ₂ III-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ F IT n n NH ₂ III-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT n n NH ₂ III-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n NH ₂ III-49-8 p-Br-Ph * H * Bz H CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table III-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ III-50-1 p-1-ph N N N Bz H CH ₃ F IT N N NH ₂ III-50-2 p-1-ph N N CH ₃ Bz H CH ₃ F IT N N NH ₂ III-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N NH ₂ III-50-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n n NH ₂ III-50-5 p-1-ph N N CH ₂ Ph Bz H CH ₃ F IT n n NH ₂ III-50-6 p-1-ph N N CH ₂ -indol-3-yl Bz H CH ₃ F IT n n NH ₂ III-50-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F it n n NH ₂ III-50-8 p-1-ph * N * Bz H CH ₃ F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) s to form a five-membered ring.

Table IV-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-1-1 CH ₃ N n n CH ₃ N F F IT N n NH ₂ IV-1-2 CH ₃ N n CH ₃ CH ₃ N F F IT N n NH ₂ IV-1-3 CH ₃ n n CH (CH ₃ ) ₂ CH ₃ N F F IT N n NH ₂ IV-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT N n NH ₂ Iv-l-s CH ₃ n n CH ₂ Ph CH ₃ N F F IT N n NH ₂ IV-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ N F F IT N n NH ₂ IV-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT n n NH ₂ IV-1-8 CH ₃ * n * CH ₃ N F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-2-1 Et H H H CH ₃ N F F IT n n NH ₂ IV-2-2 Et H H CH ₃ CH ₃ N F F IT n n NH ₂ IV-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N F F it n n NH ₂ IV-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F it n n NH ₂ IV-2-5 Et H H CH ₂ Ph CH ₃ N F F it n n NH ₂ IV-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N F F it n n NH ₂ IV-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F it n n NH ₂ IV-2-8 Et * H CH ₃ N F F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-3-1 ⁱ Pr N n H CH ₃ N F F IT N N NH ₂ IV-3-2 ⁱ Pr N n CH ₃ CH ₃ N F F IT N N NH ₂ IV-3-3 ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ N F F IT n N NH ₂ IV-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT n N NH ₂ IV-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ N F F IT n n NH ₂ IV-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ N F F IT n n NH ₂ IV-3-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT n n NH ₂ IV-3-8 ⁱ Pr * n * CH ₃ n F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-4-1 ^t Bu N n n CH ₃ n CH ₃ F IT N N NH ₂ IV-4-2 ^t Bu N n CH ₃ CH ₃ n CH ₃ F IT N N NH ₂ IV-4-3 ^t Bu N n CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n N NH ₂ IV-4-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n N NH ₂ IV-4-5 ^t Bu n n CH ₂ Ph CH ₃ n CH ₃ F IT n n NH ₂ IV-4-6 ^t Bu n n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT n n NH ₂ IV-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT n n NH ₂ IV-4-8 ^t Bu * n * CH ₃ n CH ₃ F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-5-1 Ph H H H CH ₃ n F F IT n n NH ₂ IV-5-2 Ph H H CH ₃ CH ₃ n F F IT n n NH ₂ IV-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT n n NH ₂ IV-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F it n n NH ₂ IV-5-5 Ph H H CH ₂ Ph CH ₃ n F F it n n NH ₂ IV-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n F F it n n NH ₂ IV-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F it n n NH ₂ IV-5-8 Ph * H * CH ₃ n F F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-6-1 p-me-ph H H H CH ₃ N F F IT N n NH ₂ IV-6-2 p-me-ph H H CH ₃ CH ₃ n F F IT N n NH ₂ IV-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT N n NH ₂ IV-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT N n NH ₂ IV-6-5 p-me-ph H H CH ₂ Ph CH ₃ n F F IT N n NH ₂ IV-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n F F IT n n NH ₂ IV-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n NH ₂ IV-6-8 p-me-ph * H * CH ₃ n F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-7-1 p-f-ph H H H CH ₃ n F F IT N N NH ₂ IV-7-2 p-f-ph H H CH ₃ CH ₃ n F F IT N N NH ₂ IV-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT n N NH ₂ IV-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n N NH ₂ IV-7-6 p-f-ph H H CH ₂ Ph CH ₃ n F F IT n n NH ₂ IV-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n F F IT n n NH ₂ IV-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n NH ₂ IV-7-20 p-f-ph * H * CH ₃ n F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-8-1 p-Cl-Ph H H H CH ₃ N F F IT N n NH ₂ IV-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F F IT N n NH ₂ IV-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT N n NH ₂ IV-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT N n NH ₂ IV-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N F F IT N n NH ₂ IV-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N F F IT n n NH ₂ IV-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT n n NH ₂ IV-8-8 p-Cl-Ph * H * CH ₃ N F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-9-1 p-Br-Ph H H H CH ₃ N F F IT N n NH ₂ IV-9-2 p-Br-Ph H H CH ₃ CH ₃ N F F IT N n NH ₂ IV-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT n n NH ₂ IV-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n n NH ₂ IV-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n F F IT n n NH ₂ IV-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n F F IT n n NH ₂ IV-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n NH ₂ IV-9-20 p-Br-Ph * H * CH ₃ n F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-10-1 p-1-ph N N N CH ₃ N F F IT N N NH ₂ IV-10-2 p-1-ph N N CH ₃ CH ₃ N F F IT N N NH ₂ IV-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N F F IT N n NH ₂ IV-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT N n NH ₂ IV-10-5 p-1-ph N n CH ₂ Ph CH ₃ N F F IT N n NH ₂ IV-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ N F F IT N n NH ₂ IV-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT N n NH ₂ IV-10-8 p-1-ph n * CH ₃ N F F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table GU-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-11-1 CH ₃ N n H Et H F F OH H H NH ₂ IV-11-2 CH ₃ N n CH ₃ Et H F F OH H H NH ₂ IV-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-11-5 CH ₃ N n CH ₂ Ph Et H F F OH H H NH ₂ IV-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-11-8 CH ₃ * n * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-12-1 Et H H H Et H F F OH H H NH ₂ IV-12-2 Et H H CH ₃ Et H F F OH H H NH ₂ IV-12-3 Et H H CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-12-5 Et H H CH ₂ Ph Et H F F OH H H NH ₂ IV-12-6 Et H H CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-12-8 Et * H * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-13-1 ⁱ Pr N N H Et H F F OH H H NH ₂ IV-13-2 ⁱ Pr N n CH ₃ Et H F F OH H H NH ₂ IV-13-3 ⁱ Pr N n CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-13-5 ⁱ Pr N n CH ₂ Ph Et H F F OH H H NH ₂ IV-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-13-8 ⁱ Pr * n * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-14-1 ^t bu N n H Et H F F OH H H NH ₂ IV-14-2 ^t bu n n CH ₃ Et H F F OH H H NH ₂ IV-14-3 ^t bu n n CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-14-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-14-5 ^t bu n n CH ₂ Ph Et H F F OH H H NH ₂ IV-14-6 ^t bu n n CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-14-8 ^t bu * n * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-15-1 Ph H H H Et H F F OH H H NH ₂ IV-15-2 Ph H H CH ₃ Et H F F OH H H NH ₂ IV-15-3 Ph H H CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-15-5 Ph H H CH ₂ Ph Et H F F OH H H NH ₂ IV-15-6 Ph H H CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-15-8 Ph * H * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-16-1 p-me-ph H H H Et H F F OH H H NH ₂ IV-16-2 p-me-ph H H CH ₃ Et H F F OH H H NH ₂ IV-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-16-5 p-me-ph H H CH ₂ Ph Et H F F OH H H NH ₂ IV-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-16-8 p-me-ph * H * Et H F F OH H H NH ₂

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-17-1 p-f-ph H H H Et H F F OH H H NH ₂ IV-17-2 p-f-ph H H CH ₃ Et H F F OH H H NH ₂ IV-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-17-5 p-f-ph H H CH ₂ Ph Et H F F OH H H NH ₂ IV-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-17-8 p-f-ph * H * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-18-1 p-Cl-Ph H H H Et H F F OH H H NH ₂ IV-18-2 p-Cl-Ph H H CH ₃ Et H F F OH H H NH ₂ IV-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-18-5 p-Cl-Ph H H CH ₂ Ph Et H F F OH H H NH ₂ IV-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-18-8 p-Cl-Ph * H * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table TV-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-19-1 p-Br-Ph H H H Et H F F OH H H NH ₂ IV-19-2 p-Br-Ph H H CH ₃ Et H F F OH H H NH ₂ IV-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-19-5 p-Br-Ph H H CH ₂ Ph Et H F F OH H H NH ₂ IV-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-19-8 p-Br-Ph * H * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-20-1 p-1-ph N N n Et H F F OH H H NH ₂ IV-20-2 p-1-ph N N CH ₃ Et H F F OH H H NH ₂ IV-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H NH ₂ IV-20-5 p-1-ph N n CH ₂ Ph Et H F F OH H H NH ₂ IV-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H F F OH H H NH ₂ IV-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H F F OH H H NH ₂ IV-20-8 p-1-ph * n * Et H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-21-1 CH ₃ N n n ⁱ Pr H F F OH H H NH ₂ IV-21-2 CH ₃ N n CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-21-5 CH ₃ n n CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-21-6 CH ₃ n n CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-21-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-21-8 CH ₃ * n * ⁱ Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-22-1 Et H H H ⁱ Pr H F F OH H H NH ₂ IV-22-2 Et H H CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-22-5 Et H H CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-22-8 Et * H * ⁱ Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-23-1 ⁱ Pr N N n ⁱ Pr N F F IT N n NH ₂ IV-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N F F IT N n NH ₂ IV-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr n F F IT N n NH ₂ IV-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F F IT n n NH ₂ IV-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr n F F IT n n NH ₂ IV-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr n F F IT n n NH ₂ IV-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F F IT n n NH ₂ IV-23-8 ⁱ Pr * n ⁱ Pr n F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-24-1 ^t bu N N n ⁱ Pr N F F IT N N NH ₂ IV-24-2 ^t bu N N CH ₃ ⁱ Pr N F F IT N N NH ₂ IV-24-3 ^t bu N n CH (CH ₃ ) ₂ ⁱ Pr N F F IT n N NH ₂ IV-24-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT n N NH ₂ IV-24-5 ^t bu N n CH ₂ Ph ⁱ Pr N F F IT n n NH ₂ IV-24-6 ^t bu N n CH ₂ -indol-3-yl ⁱ Pr N F F IT n n NH ₂ IV-24-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT n n NH ₂ IV-24-8 ^t bu n ⁱ Pr N F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-25-1 Ph H H H ⁱ Pr H F F OH H H NH ₂ IV-25-2 Ph H H CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-25-5 Ph H H CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-25-8 Ph H * ⁱ Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-26-1 p-me-ph H H H ⁱ Pr H F F OH H H NH ₂ IV-26-2 p-me-ph H H CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-26-8 p-me-ph * H * * Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-27-1 p-f-ph H H H ⁱ Pr H F F OH H H NH ₂ IV-27-2 p-f-ph H H CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-27-8 p-f-ph * H * ⁱ Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-28-1 p-Cl-Ph H H H ⁱ Pr H F F OH H H NH ₂ IV-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-28-8 p-Cl-Ph * H * ⁱ Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-29-1 p-Br-Ph H H H ⁱ Pr H F F OH H H NH ₂ IV-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F F OH H H NH ₂ IV-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H NH ₂ IV-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F F OH H H NH ₂ IV-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H NH ₂ IV-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H NH ₂ IV-29-8 p-Br-Ph * H * ⁱ Pr H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-30-1 p-1-ph N N n ⁱ Pr N F F IT N N NH ₂ IV-30-2 p-1-ph N N CH ₃ ⁱ Pr N F F IT N N NH ₂ IV-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr N F F IT n N NH ₂ IV-30-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT n N NH ₂ IV-30-5 p-1-ph N N CH ₂ Ph ⁱ Pr N F F IT n n NH ₂ IV-30-6 p-1-ph N N CH ₂ -indol-3-yl ⁱ Pr N F F IT n n NH ₂ IV-30-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT n n NH ₂ IV-30-8 p-1-ph * N * ⁱ Pr N F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-31-1 CH ₃ N N N ⁿ Bu H F F OH H H NH ₂ IV-31-2 CH ₃ N N CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-31-8 CH ₃ * N * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-32-1 Et H H H ⁿ Bu H F F OH H H NH ₂ IV-32-2 Et H H CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-32-5 Et H H CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-32-8 Et * H * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) s to form a five-membered ring. Table IV-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-33-1 ⁱ Pr N N N ⁿ Bu H F F OH H H NH ₂ IV-33-2 ⁱ Pr N N CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-33-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-33-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-33-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-33-8 ⁱ Pr * N ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) s to form a five-membered ring. Table IV-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-34-1 ^t bu N N n ^t bu N F F IT N n NH ₂ IV-34-2 ^t bu N N CH ₃ ^t bu n F F IT N n NH ₂ IV-34-3 ^t bu N N CH (CH ₃ ) ₂ ^t bu n F F IT n n NH ₂ IV-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ^t bu n F F IT n n NH ₂ IV-34-5 ^t bu N n CH ₂ Ph ^t bu n F F IT n n NH ₂ IV-34-6 ^t bu N n CH ₂ -indol-3-yl ^t bu n F F IT n n NH ₂ IV-34-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ^t bu n F F IT n n NH ₂ IV-34-8 ^t bu * n * ^t bu n F F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-35-1 Ph H H H ⁿ Bu H F F OH H H NH ₂ IV-35-2 Ph H H CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-35-5 Ph H H CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-35-8 Ph * H * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-36-1 p-me-ph H H H ⁿ Bu H F F OH H H NH ₂ IV-36-2 p-me-ph H H CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-36-8 p-me-ph * H * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-37-1 p-f-ph H H H ⁿ Bu H F F OH H H NH ₂ IV-37-2 p-f-ph H H CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-37-8 p-f-ph * H * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-38-1 p-Cl-Ph H H H ⁿ Bu H F F OH H H NH ₂ IV-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-38-8 p-Cl-Ph * H * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-39-1 p-Br-Ph H H H ⁿ Bu H F F OH H H NH ₂ IV-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-39-8 p-Br-Ph * H * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-40-1 p-1-ph N N H ⁿ Bu H F F OH H H NH ₂ IV-40-2 p-1-ph N N CH ₃ ⁿ Bu H F F OH H H NH ₂ IV-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-40-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H NH ₂ IV-40-5 p-1-ph N N CH ₂ Ph ⁿ Bu H F F OH H H NH ₂ IV-40-6 p-1-ph N N CH ₂ -indol-3-yl ⁿ Bu H F F OH H H NH ₂ IV-40-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H NH ₂ IV-40-8 p-1-ph * n * ⁿ Bu H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-41-1 CH ₃ N N N Bz H F F OH H H NH ₂ IV-41-2 CH ₃ N N CH ₃ Bz H F F OH H H NH ₂ IV-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-41-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-41-5 CH ₃ N N CH ₂ Ph Bz H F F OH H H NH ₂ IV-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-41-8 CH ₃ * n * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-42-1 Et H H H Bz H F F OH H H NH ₂ IV-42-2 Et H H CH ₃ Bz H F F OH H H NH ₂ IV-42-3 Et H H CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ ,. IV-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-42-5 Et H H CH ₂ Ph Bz H F F OH H H NH ₂ IV-42-6 Et H H CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-42-8 Et * H * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table TV-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-43-1 ⁱ Pr N N N Bz H F F OH H H NH ₂ IV-43-2 ⁱ Pr N N CH ₃ Bz H F F OH H H NH ₂ IV-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-43-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-43-5 ⁱ Pr N N CH ₂ Ph Bz H F F OH H H NH ₂ IV-43-6 ⁱ Pr N N CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-43-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-43-8 ⁱ Pr * N * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-44-1 ^t bu N n n Bz H F F OH H H NH ₂ IV-44-2 ^t bu N n CH ₃ Bz H F F OH H H NH ₂ IV-44-3 ^t bu N n CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-44-5 ^t bu N n CH ₂ Ph Bz H F F OH H H NH ₂ IV-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-44-8 ^t bu * n * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-45-1 Ph H H H Bz H F F OH H H NH ₂ IV-45-2 Ph H H CH ₃ Bz H F F OH H H NH ₂ IV-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-45-5 Ph H H CH ₂ Ph Bz H F F OH H H NH ₂ IV-45-6 Ph H H CH ₂ -indole-3 -yl Bz H F F OH H H NH ₂ IV-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-45-8 Ph * H * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-46-1 p-me-ph H H H Bz H F F OH H H NH ₂ IV-46-2 p-me-ph H H CH ₃ Bz H F F OH H H NH ₂ IV-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-46-5 p-me-ph H H CH ₂ Ph Bz H F F OH H H NH ₂ IV-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-46-8 p-me-ph * H * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IV-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-47-1 p-f-ph H H H Bz H F F OH H H NH ₂ IV-47-2 p-f-ph H H CH ₃ Bz H F F OH H H NH ₂ IV-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-47-5 p-f-ph H H CH ₂ Ph Bz H F F OH H H NH ₂ IV-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-47-8 p-f-ph * H * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-48-1 p-Cl-Ph H H H Bz H F F OH H H NH ₂ IV-48-2 p-Cl-Ph H H CH ₃ Bz H F F OH H H NH ₂ GU-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F F OH H H NH ₂ IV-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-48-8 p-Cl-Ph * H * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IV-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-49-1 p-Br-Ph H H H Bz H F F OH H H NH ₂ IV-49-2 p-Br-Ph H H CH ₃ Bz H F F OH H H NH ₂ IV-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-49-5 p-Br-Ph H H CH ₂ Ph Bz H F F OH H H NH ₂ IV-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-49-8 p-Br-Ph * H * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CHg) s to form a five-membered ring.

Table IY-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ IV-50-1 p-1-ph N N H Bz H F F OH H H NH ₂ IV-50-2 p-1-ph N N CH ₃ Bz H F F OH H H NH ₂ IV-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H NH ₂ IV-50-5 p-1-ph N n CH ₂ Ph Bz H F F OH H H NH ₂ IV-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H F F OH H H NH ₂ IV-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H F F OH H H NH ₂ IV-50-8 p-1-ph n * Bz H F F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-1-1 CH ₃ N N n CH ₃ N N F IT N n NH ₂ V-1-2 CH ₃ N N CH ₃ CH ₃ N N F IT N n NH ₂ V-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N N F IT N n NH ₂ V-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT N n NH ₂ V-1-5 CH ₃ N N CH ₂ Ph CH ₃ N n F IT N n NH ₂ V-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N n F IT N n NH ₂ V-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT N n NH ₂ V-1-8 CH ₃ * n * CH ₃ N n F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-2-1 Et N N n CH ₃ N N F IT N N NH ₂ V-2-2 Et N N CH ₃ CH ₃ N N F IT N N NH ₂ V-2-3 Et N n CH (CH ₃ ) ₂ CH ₃ N N F IT n N NH ₂ V-2-4 Et N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT n N NH ₂ V-2-5 Et N n CH ₂ Ph CH ₃ N N F IT n n NH ₂ V-2-6 Et N n CH ₂ -indol-3-yl CH ₃ N N F IT n n NH ₂ V-2-7 Et N n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n NH ₂ V-2-8 Et * n * CH ₃ N N F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-3-1 ^t Pr N N n CH ₃ N N F IT N n NH ₂ V-3-2 ^t Pr N N CH ₃ CH ₃ N N F IT N n NH ₂ V-3-3 ^t Pr N N CH (CH ₃ ) ₂ CH ₃ N n F IT n n NH ₂ V-3-4 ^t Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT n n NH ₂ V-3-5 ^t Pr N n CH ₂ Ph CH ₃ N n F IT n n NH ₂ V-3-6 ^t Pr N n CH ₂ -indol-3-yl CH ₃ N n F IT n n NH ₂ V-3-7 ^t Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT n n NH ₂ V-3-8 ^t Pr * n * CH ₃ N n F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-4-1 ^t Bu N n n CH ₃ N N F IT N N NH ₂ V-4-2 ^t Bu N n CH ₃ CH ₃ N N F IT N N NH ₂ V-4-3 ^t Bu N n CH (CH ₃ ) ₂ CH ₃ N N F IT n N NH ₂ V-4-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT n n NH ₂ V-4-5 ^t Bu N n CH ₂ Ph CH ₃ N N F IT n n NH ₂ V-4-6 ^t Bu N n CH ₂ -indol-3-yl CH ₃ N N F IT n n NH ₂ V-4-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n NH ₂ V-4-8 ^t Bu * n * CH ₃ N N F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-5-1 Ph H H H CH ₃ H H F OH H H NH ₂ V-5-2 Ph H H CH ₃ CH ₃ H H F OH H H NH ₂ V-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH H H NH ₂ V-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH H H NH ₂ V-5-5 Ph H H CH ₂ Ph CH ₃ H H F OH H H NH ₂ V-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ H H F OH H H NH ₂ V-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH H H NH ₂ V-5-8 Ph * H * CH ₃ H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-6-1 p-me-ph H H H CH ₃ H H F OH H H NH ₂ V-6-2 p-me-ph H H CH ₃ CH ₃ H H F OH H H NH ₂ V-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH H H NH ₂ V-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH H H NH ₂ V-6-5 p-me-ph H H CH ₂ Ph CH ₃ H H F OH H H NH ₂ V-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ H H F OH H H NH ₂ V-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH H H NH ₂ V-6-8 p-me-ph * H * CH ₃ H H F OH H H NH ₂ * R2 and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-7-1 p-f-ph H H H CH ₃ N N F IT N N NH ₂ V-7-2 p-f-ph H H CH ₃ CH ₃ N N F IT N N NH ₂ V-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT N n NH ₂ V-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT N n NH ₂ V-7-6 p-f-ph H H CH ₂ Ph CH ₃ N N F IT N n NH ₂ V-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N N F IT N n NH ₂ V-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT N n NH ₂ V-7-20 p-f-ph * H * CH ₃ N N F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-8-1 p-Cl-Ph H H H CH ₃ n N F IT n n NH ₂ V-8-2 p-Cl-Ph H H CH ₃ CH ₃ n n F IT n n NH ₂ V-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n n F IT n n NH ₂ V-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F it n n NH ₂ V-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n n F it n n NH ₂ V-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n n F it n n NH ₂ V-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F it n n NH ₂ V-8-8 p-Cl-Ph * H * CH ₃ n n F it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-9-1 p-Br-Ph H H H CH ₃ N n F IT N N NH ₂ V-9-2 p-Br-Ph H H CH ₃ CH ₃ n n F IT N N NH ₂ V-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ n n F IT N N NH ₂ V-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT N n NH ₂ V-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n n F IT N n NH ₂ V-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n n F IT N n NH ₂ V-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT N n NH ₂ V-9-20 p-Br-Ph * H * CH ₃ n n F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. * Table V-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-10-1 p-1-ph N n n CH ₃ N N F IT N n NH ₂ V-10-2 p-1-ph N n CH ₃ CH ₃ N N F IT N n NH ₂ V-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ N N F IT N n NH ₂ V-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT N n NH ₂ V-10-5 p-1-ph N n CH ₂ Ph CH ₃ N N F IT n n NH ₂ V-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ N N F IT n n NH ₂ V-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n NH ₂ V-10-8 p-1-ph * n * CH ₃ N N F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-11-1 CH ₃ N n n Et H H F OH H H NH ₂ V-11-2 CH ₃ N N CH ₃ Et H H F OH H H NH ₂ V-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-11-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-11-5 CH ₃ N N CH ₂ Ph Et H H F OH H H NH ₂ V-11-6 CH ₃ N N CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-11-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-11-8 CH ₃ * N * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-12-1 Et H H H Et H H F OH H H NH ₂ V-12-2 Et H H CH ₃ Et H H F OH H H NH ₂ V-12-3 Et H H CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-12-5 Et H H CH ₂ Ph Et H H F OH H H NH ₂ V-12-6 Et H H CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-12-8 Et * H * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-13-1 ⁱ Pr N N n Et H H F OH H H NH ₂ V-13-2 ⁱ Pr N N CH ₃ Et H H F OH H H NH ₂ V-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-13-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-13-5 ⁱ Pr N N CH ₂ Ph Et H H F OH H H NH ₂ V-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-13-8 ⁱ Pr * n * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-14-1 ^t bu N n n Et H H F OH H H NH ₂ V-14-2 ^t bu N n CH ₃ Et H H F OH H H NH ₂ V-14-3 ^t bu n n CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-14-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-14-5 ^t bu n n CH ₂ Ph Et H H F OH H H NH ₂ V-14-6 ^t bu n n CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-14-8 ^t bu * n Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-15-1 Ph H H H Et H H F OH H H NH ₂ V-15-2 Ph H H CH ₃ Et H H F OH H H NH ₂ V-15-3 Ph H H CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-1s-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-15-5 Ph H H CH ₂ Ph Et H H F OH H H NH ₂ V-15-6 Ph H H CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-15-8 Ph * H Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-16-1 p-me-ph H H H Et H H F OH H H NH ₂ V-16-2 p-me-ph H H CH ₃ Et H H F OH H H NH ₂ V-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-16-5 p-me-ph H H CH ₂ Ph Et H H F OH H H NH ₂ V-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-16-8 p-me-ph * H * Et H H F OH H H NH ₂

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-17-1 p-f-ph H H H Et H H F OH H H NH ₂ V-17-2 p-f-ph H H CH ₃ Et H H F OH H H NH ₂ V-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-17-5 p-f-ph H H CH ₂ Ph Et H H F OH H H NH ₂ V-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-17-8 p-f-ph H * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-18-1 p-Cl-Ph H H H Et H H F OH H H NH ₂ V-18-2 p-Cl-Ph H H CH ₃ Et H H F OH H H NH ₂ V-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-18-5 p-Cl-Ph H H CH ₂ Ph Et H H F OH H H NH ₂ V-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-18-8 p-Cl-Ph H * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-19-1 p-Br-Ph H H H Et H H F OH H H NH ₂ V-19-2 p-Br-Ph H H CH ₃ Et H H F OH H H NH ₂ V-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-19-5 p-Br-Ph H H CH ₂ Ph Et H H F OH H H NH ₂ V-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-19-8 p-Br-Ph * H * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-20-1 p-1-ph N n n Et H H F OH H H NH ₂ V-20-2 p-1-ph N n CH ₃ Et H H F OH H H NH ₂ V-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H NH ₂ V-20-5 p-1-ph N n CH ₂ Ph Et H H F OH H H NH ₂ V-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H H F OH H H NH ₂ V-20-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Et H H F OH H H NH ₂ V-20-8 p-1-ph * n * Et H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-21-1 CH ₃ N N n ⁱ Pr N N F IT N n NH ₂ V-21-2 CH ₃ N N CH ₃ ⁱ Pr N N F IT N n NH ₂ V-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N n F IT N n NH ₂ V-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N n F IT N n NH ₂ V-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N n F IT N n NH ₂ V-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N n F IT N n NH ₂ V-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N n F IT N n NH ₂ V-21-8 CH ₃ * n ⁱ Pr N n F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-22-1 Et H H H ⁱ Pr H H F OH H H NH ₂ V-22-2 Et H H CH ₃ ⁱ Pr H H F OH H H NH ₂ V-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-22-5 Et H H CH ₂ Ph ⁱ Pr H H F OH H H NH ₂ V-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H NH ₂ V-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H NH ₂ V-22-8 Et * H * ⁱ Pr H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-23-1 ⁱ Pr N N n ⁱ Pr N N F IT N N NH ₂ V-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N N F IT N N NH ₂ V-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr n N F IT N N NH ₂ V-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n n F IT N N NH ₂ V-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr n n F IT N N NH ₂ V-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr n n F IT N N NH ₂ V-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n n F IT N N NH ₂ V-23-8 ⁱ Pr * n * ⁱ Pr n n F IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-24-1 ^t bu N n n ⁱ Pr N N F IT N N NH ₂ V-24-2 ^t bu N n CH ₃ ⁱ Pr N N F IT N N NH ₂ V-24-3 ^t bu n n CH (CH ₃ ) ₂ ⁱ Pr N N F IT N N NH ₂ V-24-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N N F IT N N NH ₂ V-24-5 ^t bu n n CH ₂ Ph ⁱ Pr N N F IT n n NH ₂ V-24-6 ^t bu n n CH ₂ -indol-3-yl ⁱ Pr N N F IT n n NH ₂ V-24-7 ^t bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N N F IT n n NH ₂ V-24-8 ^t bu * n * ⁱ Pr N N F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-25-1 Ph H H H ⁱ Pr H H F OH H H NH ₂ V-25-2 Ph H H CH ₃ ⁱ Pr H H F OH H H NH ₂ V-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-25-5 Ph H H CH ₂ Ph ⁱ Pr H H F OH H H NH ₂ V-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H NH ₂ V-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H NH ₂ V-25-8 Ph * H * ⁱ Pr H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-26-1 p-me-ph H H H ⁱ Pr H H F OH H H NH ₂ V-26-2 p-me-ph H H CH ₃ ⁱ Pr H H F OH H H NH ₂ V-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ H H F OH H H NH ₂ V-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H H F OH H H NH ₂ V-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H NH ₂ V-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H NH ₂ V-26-8 p-me-ph * H * ⁱ Pr H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-27-1 p-f-ph H H H ⁱ Pr H H F OH H H NH ₂ V-27-2 p-f-ph H H CH ₃ ⁱ Pr H H F OH H H NH ₂ V-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H H F OH H H NH ₂ V-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H NH ₂ V-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H NH ₂ V-27-8 p-f-ph * H * ⁱ Pr H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-28-1 p-Cl-Ph H H H ⁱ Pr H H F OH H H NH ₂ V-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H H F OH H H NH ₂ V-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H H F OH H H NH ₂ V-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H NH ₂ V-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H NH ₂ V-28-8 p-Cl-Ph * H * ⁱ Pr H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-29-1 p-Br-Ph H H H ⁱ Pr H H F OH H H NH ₂ V-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H H F OH H H NH ₂ V-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H NH ₂ V-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H H F OH H H NH ₂ V-29-6 p-Br-Ph H H CH ₂ -indole-3-IL ⁱ Pr H H F OH H H NH ₂ V-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H NH ₂ V-29-8 p-Br-Ph * H * ⁱ Pr H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-30-1 p-1-ph N N n ⁱ Pr N N F IT N N NH ₂ V-30-2 p-1-ph N N CH ₃ ⁱ Pr N N F IT N N NH ₂ V-30-3 p-1-ph N n CH (CH ₃ ) ₂ ⁱ Pr N N F IT n N NH ₂ V-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N N F IT n n NH ₂ V-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr N N F IT n n NH ₂ V-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr N N F IT n n NH ₂ V-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N N F IT n n NH ₂ V-30-8 p-1-ph * n * ⁱ Pr N N F IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-31-1 CH ₃ N n n ⁿ Bu H H F OH H H NH ₂ V-31-2 CH ₃ N n CH ₃ ⁿ Bu H H F OH H H NH ₂ V-31-3 CH ₃ n n CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-31-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-31-5 CH ₃ n n CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-31-6 CH ₃ n n CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-31-8 CH ₃ * n * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-32-1 Et H H H ⁿ Bu H H F OH H H NH ₂ V-32-2 Et H H CH ₃ ⁿ Bu H H F OH H H NH ₂ V-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-32-5 Et H H CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-32-8 Et * H * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-33-1 ⁱ Pr N N n ⁿ Bu H H F OH H H NH ₂ V-33-2 ⁱ Pr N N sn3 ⁿ Bu H H F OH H H NH ₂ V-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-33-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-33-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-33-8 ⁱ Pr * n * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-34-1 ^t bu N N n ⁿ Bu N N F IT N N NH ₂ V-34-2 ^t bu N N CH ₃ ⁿ Bu N N F IT N N NH ₂ V-34-3 ^t bu N N CH (CH ₃ ) ₂ ⁿ Bu N N F IT N N NH ₂ V-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N N F IT N N NH ₂ V-34-5 ^t bu N n CH ₂ Ph ⁿ Bu N N F IT N N NH ₂ V-34-6 ^t bu N n CH ₂ -indol-3-yl ⁿ Bu N N F IT N N NH ₂ V-34-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N N F IT N N NH ₂ V-34-8 ^t bu * n * ⁿ Bu N N F IT N N NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-35-1 Ph H H H ⁿ Bu H H F OH H H NH ₂ V-35-2 Ph H H CH ₃ ⁿ Bu H H F OH H H NH ₂ V-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-35-5 Ph H H CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-35-8 Ph * H * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-36-1 p-me-ph H H H ⁿ Bu H H F OH H H NH ₂ V-36-2 p-me-ph H H CH ₃ ⁿ Bu H H F OH H H NH ₂ V-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-36-8 p-me-ph * H * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-37-1 p-f-ph H H H ⁿ Bu H H F OH H H NH ₂ V-37-2 p-f-ph H H CH ₃ ⁿ Bu H H F OH H H NH ₂ V-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-37-8 p-f-ph * H ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-38-1 p-Cl-Ph H H H ⁿ Bu H H F OH H H NH ₂ V-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H H F OH H H NH ₂ V-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-38-8 p-Cl-Ph * H * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-39-1 p-Br-Ph H H H ⁿ Bu H H F OH H H NH ₂ V-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H H F OH H H NH ₂ V-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-39-8 p-Br-Ph * H * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-40-1 p-1-ph N N n ⁿ Bu H H F OH H H NH ₂ V-40-2 p-1-ph N n CH ₃ ⁿ Bu H H F OH H H NH ₂ V-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H NH ₂ V-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H H F OH H H NH ₂ V-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H H F OH H H NH ₂ V-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H NH ₂ V-40-8 p-1-ph * n * ⁿ Bu H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-41-1 CH ₃ N N n Bz H H F OH H H NH ₂ V-41-2 CH ₃ N N CH ₃ Bz H H F OH H H NH ₂ V-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-41-5 CH ₃ N n CH ₂ Ph Bz H H F OH H H NH ₂ V-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-41-8 CH ₃ * n * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-42-1 Et H H H Bz H H F OH H H NH ₂ V-42-2 Et H H CH ₃ Bz H H F OH H H NH ₂ V-42-3 Et H H CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-42-5 Et H H CH ₂ Ph Bz H H F OH H H NH ₂ V-42-6 Et H H CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-42-8 Et * H * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-43-1 ⁱ Pr N N n Bz H H F OH H H NH ₂ V-43-2 ⁱ Pr N N CH ₃ Bz H H F OH H H NH ₂ V-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-43-5 ⁱ Pr N n CH ₂ Ph Bz H H F OH H H NH ₂ V-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-43-8 ⁱ Pr * n * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-44-1 ^t bu N n n Bz H H F OH H H NH ₂ V-44-2 ^t bu N n CH ₃ Bz H H F OH H H NH ₂ V-44-3 ^t bu N n CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-44-5 ^t bu N n CH ₂ Ph Bz H H F OH H H NH ₂ V-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-44-8 ^t bu * n * Bz H H F OH H H NH ₂ * R ² and R ^3b b are connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-45-1 Ph H H H Bz H H F OH H H NH ₂ V-45-2 Ph H H CH ₃ Bz H H F OH H H NH ₂ V-45-3 Ph H H CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-45-5 Ph H H CH ₂ Ph Bz H H F OH H H NH ₂ V-45-6 Ph H H CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-45-8 Ph * H * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-46-1 p-me-ph H H H Bz H H F OH H H NH ₂ V-46-2 p-me-ph H H CH ₃ Bz H H F OH H H NH ₂ V-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-46-5 p-me-ph H H CH ₂ Ph Bz H H F OH H H NH ₂ V-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-46-8 p-me-ph * H * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) 3 to form a five-membered ring.

Table V-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-47-1 p-f-ph H H H Bz H H F OH H H NH ₂ V-47-2 p-f-ph H H CH ₃ Bz H H F OH H H NH ₂ V-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-47-5 p-f-ph H H CH ₂ Ph Bz H H F OH H H NH ₂ V-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-47-8 p-f-ph * H Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-48-1 p-Cl-Ph H H H Bz H H F OH H H NH ₂ V-48-2 p-Cl-Ph H H CH ₃ Bz H H F OH H H NH ₂ V-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-48-5 p-Cl-Ph H H CH ₂ Ph Bz H H F OH H H NH ₂ V-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-48-8 p-Cl-Ph * H * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table V-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-49-1 p-Br-Ph H H H Bz H H F OH H H NH ₂ V-49-2 p-Br-Ph H H CH ₃ Bz H H F OH H H NH ₂ V-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-49-5 p-Br-Ph H H CH ₂ Ph Bz H H F OH H H NH ₂ V-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-49-8 p-Br-Ph * H * Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table V-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ V-50-1 p-1-ph N n n Bz H H F OH H H NH ₂ V-50-2 p-1-ph N n CH ₃ Bz H H F OH H H NH ₂ V-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-50-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H NH ₂ V-50-5 p-1-ph n n CH ₂ Ph Bz H H F OH H H NH ₂ V-50-6 p-1-ph n n CH ₂ -indol-3-yl Bz H H F OH H H NH ₂ V-50-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H NH ₂ V-50-8 p-1-ph * n Bz H H F OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-1-1 CH ₃ N n n CH ₃ N F N IT n n VI-1-2 CH ₃ N n CH ₃ CH ₃ N F N IT n n VI-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N F n IT n n VI-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-1-5 CH ₃ n n CH ₂ Ph CH ₃ N F n it n n VI-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ N F n it n n VI-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n VI-1-8 CH ₃ * n * CH ₃ N F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-2-1 Et H H H CH ₃ H F H OH H H VI-2-2 Et H H CH ₃ CH ₃ H F H OH H H VI-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H F H OH H H VI-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F H OH H H VI-2-5 Et H H CH ₂ Ph CH ₃ H F H OH H H VI-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H F H OH H H VI-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H F H OH H H VI-2-8 Et * H * CH ₃ H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-3-1 ⁱ Pr N N N CH ₃ N F n IT n n VI-3-2 ⁱ Pr N N CH ₃ CH ₃ N F n IT n n VI-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ n F n it n n VI-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it n n VI-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ n F n it n n VI-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ n F n it n n VI-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n F n it n n VI-3-8 ^t Pr * H * CH ₃ H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-4-1 ^t bu N n n CH ₃ N F n IT n n VI-4-2 ^t bu N n CH ₃ CH ₃ N F n IT n n VI-4-3 ^t bu N n CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-4-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-4-5 ^t bu n n CH ₂ Ph CH ₃ N F n it n n VI-4-6 ^t bu n n CH ₂ -indol-3-yl CH ₃ n F n it n n VI-4-7 ^t bu n n CH ₂ CH ₂ SCH ₃ CH ₃ n F n it n n VI-4-8 ^t bu * n * CH ₃ n F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-5-1 Ph H H H CH ₃ n F N IT n n VI-5-2 Ph H H CH ₃ CH ₃ n F N it n n VI-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n F n it n n VI-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it n n VI-5-5 Ph H H CH ₂ Ph CH ₃ n F n it n n VI-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n F n it n n VI-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it n n VI-5-8 Ph * H * CH ₃ n F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-6-1 p-me-ph H H H CH ₃ N F N IT N N VI-6-2 p-me-ph H H CH ₃ CH ₃ N F N IT N N VI-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N F N IT N N VI-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT N n VI-6-5 p-me-ph H H CH ₂ Ph CH ₃ N F N IT N n VI-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N F N IT N n VI-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT N n VI-6-8 p-me-ph H * CH ₃ N F N IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-7-1 p-f-ph H H H CH ₃ N F n IT n n VI-7-2 p-f-ph H H CH ₃ CH ₃ N F n IT n n VI-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-7-6 p-f-ph H H CH ₂ Ph CH ₃ N F n it n n VI-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N F n it n n VI-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n VI-7-20 p-f-ph * H * CH ₃ N F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-8-1 p-Cl-Ph H H H CH ₃ N F N IT n N VI-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F N IT n N VI-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n F N IT n n VI-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT n n VI-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n F N IT n n VI-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n F N it n n VI-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F N it n n VI-8-8 p-Cl-Ph * H * CH ₃ n F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-9-1 p-Br-Ph H H H CH ₃ N F n IT n n VI-9-2 p-Br-Ph H H CH ₃ CH ₃ N F n IT n n VI-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it n n VI-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F n it n n VI-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N F n it n n VI-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n VI-9-20 p-Br-Ph * H * CH ₃ N F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-10-1 p-1-ph n n n CH ₃ N F n IT n n VI-10-2 p-1-ph n n CH ₃ CH ₃ N F n IT n n VI-10-3 p-1-ph n n CH (CH ₃ ) ₂ CH ₃ N F n IT n n VI-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n IT n n VI-10-5 p-1-ph n n CH ₂ Ph CH ₃ N F n IT n n VI-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N F n IT n n VI-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n VI-10-8 p-1-ph n * CH ₃ N F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-11-1 CH ₃ N n n Et H F H OH H H VI-11-2 CH ₃ N n CH ₃ Et H F H OH H H VI-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H F H OH H H VI-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-U-5 CH ₃ N n CH ₂ Ph Et H F H OH H H VI-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H F H OH H H VI-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-11-8 CH ₃ * n * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-12-1 Et H H H Et H F H OH H H VI-12-2 Et H H CH ₃ Et H F H OH H H VI-12-3 Et H H CH (CH ₃ ) ₂ Et H F H OH H H VI-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-12-5 Et H H CH ₂ Ph Et H F H OH H H VI-12-6 Et H H CH ₂ -indol-3-yl Et H F H OH H H VI-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-12-8 Et * H * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-13-1 ⁱ Pr N n n Et H F H OH H H VI-13-2 ⁱ Pr N n CH ₃ Et H F H OH H H VI-13-3 ⁱ Pr n n CH (CH ₃ ) ₂ Et H F H OH H H VI-13-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-13-5 ⁱ Pr n n CH ₂ Ph Et H F H OH H H VI-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et H F H OH H H VI-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-13-8 ⁱ Pr * n Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-14-1 ^t bu N N n Et H F H OH H H VI-14-2 ^t bu N N CH ₃ Et H F H OH H H VI-14-3 ^t bu N N CH (CH ₃ ) ₂ Et H F H OH H H VI-14-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-14-5 ^t bu N n CH ₂ Ph Et H F H OH H H VI-14-6 ^t bu N n CH ₂ -indol-3-yl Et H F H OH H H VI-14-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-14-8 ^t bu * n * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-15-1 Ph H H H Et H F H OH H H VI-15-2 Ph H H CH ₃ Et H F H OH H H VI-15-3 Ph H H CH (CH ₃ ) ₂ Et H F H OH H H VI-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-15-5 Ph H H CH ₂ Ph Et H F H OH H H VI-15-6 Ph H H CH ₂ -indol-3-yl Et H F H OH H H VI-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-15-8 Ph * H * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-16-1 p-me-ph H H H Et H F H OH H H VI-16-2 p-me-ph H H CH ₃ Et H F H OH H H VI-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F H OH H H VI-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-16-5 p-me-ph H H CH ₂ Ph Et H F H OH H H VI-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F H OH H H VI-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-16-8 p-me-ph * H * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-17-1 p-f-ph H H H Et H F H OH H H VI-17-2 p-f-ph H H CH ₃ Et H F H OH H H VI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F H OH H H VI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-17-5 p-f-ph H H CH ₂ Ph Et H F H OH H H VI-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F H OH H H VI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-17-8 p-f-ph * H * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-18-1 p-Cl-Ph H H H Et H F H OH H H VI-18-2 p-Cl-Ph H H CH ₃ Et H F H OH H H VI-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F H OH H H VI-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-18-5 p-Cl-Ph H H CH ₂ Ph Et H F H OH H H VI-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F H OH H H VI-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-18-8 p-Cl-Ph * H * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-19-1 p-Br-Ph H H H Et H F H OH H H VI-19-2 p-Br-Ph H H CH ₃ Et H F H OH H H VI-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F H OH H H VI-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-19-5 p-Br-Ph H H CH ₂ Ph Et H F H OH H H VI-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F H OH H H VI-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-19-8 p-Br-Ph * H * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-20-1 p-1-ph N N N Et H F H OH H H VI-20-2 p-1-ph N N CH ₃ Et H F H OH H H VI-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et H F H OH H H VI-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H VI-20-5 p-1-ph N n CH ₂ Ph Et H F H OH H H VI-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H F H OH H H VI-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H F H OH H H VI-20-8 p-1-ph * n * Et H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-21-1 CH ₃ N n n ⁱ Pr N F N IT n N VI-21-2 CH ₃ N n CH ₃ ⁱ Pr N F N IT n N VI-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr N F N IT n n VI-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F N IT n n VI-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N F N IT n n VI-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N F N IT n n VI-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F N IT n n VI-21-8 CH ₃ * n * ⁱ Pr N F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-22-1 Et H H H ⁱ Pr H F H OH H H VI-22-2 Et H H CH ₃ ⁱ Pr H F H OH H H VI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-22-5 Et H H CH ₂ Ph ⁱ Pr H F H OH H H VI-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H VI-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H VI-22-8 Et * H * ⁱ Pr H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-23-1 ⁱ Pr N n n ⁱ Pr N F N IT n n VI-23-2 ⁱ Pr N n CH ₃ ⁱ Pr N F N IT n n Vl-23-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁱ Pr N F n IT n n VI-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F n it n n VI-23-5 ⁱ Pr n n CH ₂ Ph ⁱ Pr N F n it n n VI-23-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr N F n it n n VI-23-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F n it n n VI-23-8 ⁱ Pr * n * ⁱ Pr N F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-24-1 ^t bu N n n ⁱ Pr N F N IT n N VI-24-2 ^t bu N n CH ₃ ⁱ Pr N F N IT n n VI-24-3 ^t bu n n CH (CH ₃ ) ₂ ⁱ Pr n F N IT n n VI-24-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F N IT n n VI-24-5 ^t bu n n CH ₂ Ph ⁱ Pr n F n it n n VI-24-6 ^t bu n n CH ₂ -indol-3-yl ⁱ Pr n F n it n n VI-24-7 ^t bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it n n VI-24-8 ^t bu * n * ⁱ Pr n F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-25-1 Ph H H H ⁱ Pr H F H OH H H VI-25-2 Ph H H CH ₃ ⁱ Pr H F H OH H H VI-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-25-5 Ph H H CH ₂ Ph ⁱ Pr H F H OH H H VI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H VI-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H VI-25-8 Ph * H * ⁱ Pr H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-26-1 p-me-ph H H H ⁱ Pr H F H OH H H VI-26-2 p-me-ph H H CH ₃ ⁱ Pr H F H OH H H VI-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F H OH H H VI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H VI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H VI-26-8 p-me-ph H * ⁱ Pr H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-27-1 p-f-ph H H H ⁱ Pr H F H OH H H VI-27-2 p-f-ph H H CH ₃ ⁱ Pr H F H OH H H VI-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F H OH H H VI-27-6 p-f-ph H H CH ₂ -IND0L-3-IL ⁱ Pr H F H OH H H VI-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H VI-27-8 p-f-ph * H * ⁱ Pr H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-28-1 p-Cl-Ph H H H ^t Pr H F H OH H H VI-28-2 p-Cl-Ph H H CH ₃ ^t Pr H F H OH H H VI-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ^t Pr H F H OH H H VI-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ^t Pr H F H OH H H VI-28-5 p-Cl-Ph H H CH ₂ Ph * Pr H F H OH H H VI-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ^t Pr H F H OH H H VI-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ * Pr H F H OH H H VI-28-8 p-Cl-Ph * H * ^t Pr H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-29-1 p-Br-Ph H H H ⁱ Pr H F H OH H H VI-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F H OH H H VI-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H VI-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F H OH H H VI-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H VI-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H VI-29-8 p-Br-Ph H * ⁱ Pr H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-30-1 p-1-ph N N N ⁱ Pr N F n IT n n VI-30-2 p-1-ph N N CH ₃ ⁱ Pr N F n IT n n VI-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr N F n it n n VI-30-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F n it n n VI-30-5 p-1-ph N N CH ₂ Ph ⁱ Pr N F n it n n VI-30-6 p-1-ph N N CH ₂ -indol-3-yl ⁱ Pr N F n it n n VI-30-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N F n it n n VI-30-8 p-1-ph * N * ⁱ Pr N F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-31-1 CH ₃ N N n ⁿ Bu H F H OH H H VI-31-2 CH ₃ N N CH ₃ ⁿ Bu H F H OH H H VI-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H F H OH H H VI-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-31-8 CH ₃ * n * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-32-1 Et H H H ⁿ Bu H F H OH H H VI-32-2 Et H H CH ₃ ⁿ Bu H F H OH H H VI-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-32-5 Et H H CH ₂ Ph ⁿ Bu H F H OH H H VI-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-32-8 Et * H * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-33-1 ⁱ Pr N N n ⁿ Bu H F H OH H H VI-33-2 ⁱ Pr N n CH ₃ ⁿ Bu H F H OH H H VI-33-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-33-5 ⁱ Pr N n CH ₂ Ph ⁿ Bu H F H OH H H VI-33-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-33-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-33-8 ⁱ Pr * n * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-34-1 ^t bu N n n ⁿ Bu H F H OH H H VI-34-2 ^t bu N n CH ₃ ⁿ Bu H F H OH H H VI-34-3 ^t bu N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-34-5 ^t bu n n CH ₂ Ph ⁿ Bu H F H OH H H VI-34-6 ^t bu n n CH ₃ -indol-3-yl ⁿ Bu H F H OH H H VI-34-7 ^t bu n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-34-8 ^t bu * n * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-35-1 Ph H H H ⁿ Bu H F H OH H H VI-35-2 Ph H H CH ₃ ⁿ Bu H F H OH H H VI-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-35-5 Ph H H CH ₂ Ph ⁿ Bu H F H OH H H VI-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-35-8 Ph * H * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-36-1 p-me-ph H H H ⁿ Bu H F H OH H H VI-36-2 p-me-ph H H CH ₃ ⁿ Bu H F H OH H H VI-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F H OH H H VI-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-36-8 p-me-ph * H * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-37-1 p-f-ph H H H ⁿ Bu H F H OH H H VI-37-2 p-f-ph H H CH ₃ ⁿ Bu H F H OH H H VI-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F H OH H H VI-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-37-8 p-f-ph H * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-38-1 p-Cl-Ph H H H ⁿ Bu H F H OH H H VI-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F H OH H H VI-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F H OH H H VI-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-38-8 p-Cl-Ph H * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-39-1 p-Br-Ph H H H ⁿ Bu H F H OH H H VI-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F H OH H H VI-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F H OH H H VT-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-39-8 p-Br-Ph * H * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-40-1 p-1-ph N n n ⁿ Bu H F H OH H H VI-40-2 p-1-ph N n CH ₃ ⁿ Bu H F H OH H H VI-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H VI-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H F H OH H H VI-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H F H OH H H VI-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H VI-40-8 p-1-ph * n * ⁿ Bu H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-41-1 CH ₃ N N n Bz H F H OH H H VI-41-2 CH ₃ N N CH ₃ Bz H F H OH H H VI-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H F H OH H H VI-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-41-5 CH ₃ N n CH ₂ Ph Bz H F H OH H H VI-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H F H OH H H VI-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-41-8 CH ₃ * n * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-42-1 Et H H H Bz H F H OH H H VI-42-2 Et H H CH ₃ Bz H F H OH H H VI-42-3 Et H H CH (CH ₃ ) ₂ Bz H F H OH H H VI-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-42-5 Et H H CH ₂ Ph Bz H F H OH H H VI-42-6 Et H H CH ₂ -indol-3-yl Bz H F H OH H H VI-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-42-8 Et * H * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-43-1 ⁱ Pr N N n Bz H F H OH H H VI-43-2 ⁱ Pr N N CH ₃ Bz H F H OH H H VI-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H F H OH H H VI-43-4 ' ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-43-5 ⁱ Pr N n CH ₂ Ph Bz H F H OH H H VI-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz H F H OH H H VI-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-43-8 ⁱ Pr * n * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-44-1 ^t bu N N n Bz H F H OH H H VI-44-2 ^t bu N N CH ₃ Bz H F H OH H H VI-44-3 ^t bu N N CH (CH ₃ ) ₂ Bz H F H OH H H VI-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-44-5 ^t bu N n CH ₂ Ph Bz H F H OH H H VI-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H F H OH H H VI-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-44-8 ^t bu * n * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-45-1 Ph H H H Bz H F H OH H H VI-45-2 Ph H H CH ₃ Bz H F H OH H H VI-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F H OH H H VI-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-45-5 Ph H H CH ₂ Ph Bz H F H OH H H VI-45-6 Ph H H CH ₂ -indol-3-yl Bz H F H OH H H VI-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-45-8 Ph * H * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-46-1 p-me-ph H H H Bz H F H OH H H VI-46-2 p-me-ph H H CH ₃ Bz H F H OH H H VI-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F H OH H H VI-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-46-5 p-me-ph H H CH ₂ Ph Bz H F H OH H H VI-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F H OH H H VI-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-46-8 p-me-ph * H * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-47-1 p-f-ph H H H Bz H F H OH H H VI-47-2 p-f-ph H H CH ₃ Bz H F H OH H H VI-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F H OH H H VI-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-47-5 p-f-ph H H CH ₂ Ph Bz H F H OH H H VI-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F H OH H H VI-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-47-8 p-f-ph * H * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-48-1 p-Cl-Ph H H H Bz H F H OH H H VI-48-2 p-Cl-Ph H H CH ₃ Bz H F H OH H H VI-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F H OH H H VI-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F H OH H H VI-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F H OH H H VI-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-48-8 p-Cl-Ph * H * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VI-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-49-1 p-Br-Ph H H H Bz H F H OH H H VI-49-2 p-Br-Ph H H CH ₃ Bz H F H OH H H VI-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F H OH H H VI-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-49-5 p-Br-Ph H H CH ₂ Ph Bz H F H OH H H VI-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F H OH H H VI-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-49-8 p-Br-Ph * H * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VI-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VI-50-1 p-1-ph N n n Bz H F H OH H H VI-50-2 p-1-ph N n CH ₃ Bz H F H OH H H VI-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz H F H OH H H VI-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H VI-50-5 p-1-ph N n CH ₂ Ph Bz H F H OH H H VI-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H F H OH H H VI-50-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H VI-50-8 p-1-ph * n * Bz H F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-1-1 CH ₃ N N n CH ₃ N F N IT N N NH ₂ VII-1-2 CH ₃ N N CH ₃ CH ₃ N F N IT N N NH ₂ VII-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N F N IT n N NH ₂ VII-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT n N NH ₂ VII-1-5 CH ₃ N N CH ₂ Ph CH ₃ N F N IT n n NH ₂ VII-1-6 CH ₃ N N CH ₂ -indol-3-yl CH ₃ N F N IT n n NH ₂ VH-1-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT n n NH ₂ VII-1-8 CH ₃ * n * CH ₃ N F N IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VH-2-1 Et H H H CH ₃ N F n IT n n NH ₂ VII-2-2 Et H H CH ₃ CH ₃ N F n IT n n NH ₂ VII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N F n it n n NH ₂ VII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it n n NH ₂ VII-2-5 Et H H CH ₂ Ph CH ₃ n F n it n n NH ₂ VII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ n F n it n n NH ₂ VII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it n n NH ₂ VII-2-8 Et * H * CH ₃ n F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-3-1 ⁱ Pr N N n CH ₃ N F N IT N n NH ₂ VII-3-2 ⁱ Pr N N CH ₃ CH ₃ n F N IT N n NH ₂ VII-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ n F N IT n n NH ₂ VII-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT n n NH ₂ VII-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ n F N IT n n NH ₂ VII-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ n F N IT n n NH ₂ VII-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT n n NH ₂ VII-3-8 ⁱ Pr * n * CH ₃ n F N IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-4-1 ^t bu N n n CH ₃ n F n IT n n NH ₂ VII-4-2 ^t bu N n CH ₃ CH ₃ n F n IT n n NH ₂ VII-4-3 ^t bu N n CH (CH ₃ ) ₂ CH ₃ n F n it n n NH ₂ VII-4-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it n n NH ₂ VII-4-5 ^t bu N n CH ₂ Ph CH ₃ n F n it n n NH ₂ VII-4-6 ^t bu N n CH ₂ -indol-3-yl CH ₃ n F n it n n NH ₂ VII-4-7 ^t bu n n CH ₂ CH ₂ SCH ₃ CH ₃ n F n it n n NH ₂ VII-4-8 ^t bu * n * CH ₃ n F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-5-1 Ph H H H CH ₃ N F n IT n n NH ₂ VII-5-2 Ph H H CH ₃ CH ₃ N F n IT n n NH ₂ VII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N F n it n n NH ₂ VII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it n n NH ₂ VII-5-5 Ph H H CH ₂ Ph CH ₃ N F n it n n NH ₂ VII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N F n it n n NH ₂ VII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n NH ₂ VII-5-8 Ph * H * CH ₃ N F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-6-1 p-me-ph H H H CH ₃ N F N IT n n NH ₂ VII-6-2 p-me-ph H H CH ₃ CH ₃ N F n IT n n NH ₂ VII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N F n IT n n NH ₂ VH-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it n n NH ₂ VII-6-5 p-me-ph H H CH ₂ Ph CH ₃ N F n it n n NH ₂ VII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N F n it n n NH ₂ VII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n NH ₂ VII-6-8 p-me-ph H * CH ₃ N F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-7-1 p-f-ph H H H CH ₃ N F N IT n N NH ₂ VII-7-2 p-f-ph H H CH ₃ CH ₃ N F N IT n n NH ₂ VII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N F N IT n n NH ₂ VII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT n n NH ₂ VII-7-6 p-f-ph H H CH ₂ Ph CH ₃ N F N it n n NH ₂ VII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N F N it n n NH ₂ VII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n NH ₂ VII-7-20 p-f-ph H * CH ₃ n F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-8-1 p-Cl-Ph H H H CH ₃ n F n IT n n NH ₂ VII-8-2 p-Cl-Ph H H CH ₃ CH ₃ n F n IT n n NH ₂ VII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n F n it n n NH ₂ VII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it n n NH ₂ VII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n F n it n n NH ₂ VII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n F n it n n NH ₂ VII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it n n NH ₂ VTI-8-8 p-Cl-Ph * H * CH ₃ n F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-9-1 p-Br-Ph H H H CH ₃ N F N IT N N NH ₂ VII-9-2 p-Br-Ph H H CH ₃ CH ₃ N F N it N N NH ₂ VII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F N it n N NH ₂ VII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT n N NH ₂ VII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n F N IT n n NH ₂ VII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n F N IT n n NH ₂ VII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT n n NH ₂ VII-9-20 p-Br-Ph * H CH ₃ n F N IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-10-1 p-1-ph N N n CH ₃ N F n IT n n NH ₂ VII-10-2 p-1-ph N N CH ₃ CH ₃ N F n IT n n NH ₂ VII-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N F n IT n n NH ₂ VII-10-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n IT n n NH ₂ VII-10-5 p-1-ph N N CH ₂ Ph CH ₃ N F n it n n NH ₂ VII-10-6 p-1-ph N N CH ₂ -indol-3-yl CH ₃ N F n it n n NH ₂ VII-10-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ CH ₃ N F n it n n NH ₂ VII-10-8 p-1-ph * N * CH ₃ N F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-11. No. R R R3a R ^3b R R Rb X Y R ' R Ry VII-11-1 CH ₃ N N n Et H F H OH H H NH ₂ VII-11-2 CH ₃ N N CH ₃ Et H F H OH H H NH ₂ VII-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-11-5 CH ₃ N n CH ₂ Ph Et H F H OH H H NH ₂ VII-11-6 CH ₃ n n CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-11-8 CH ₃ * n Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-12-1 Et H H H Et H F H OH H H NH ₂ VII-12-2 Et H H CH ₃ Et H F H OH H H NH ₂ VII-12-3 Et H H CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-12-5 Et H H CH ₂ Ph Et H F H OH H H NH ₂ VII-12-6 Et H H CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-12-8 Et H * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-13-1 ⁱ Pr N n n Et H F H OH H H NH ₂ VII-13-2 ⁱ Pr N n CH ₃ Et H F H OH H H NH ₂ VII-13-3 ⁱ Pr N n CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-13-5 ⁱ Pr N n CH ₂ Ph Et H F H OH H H NH ₂ VII-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VH-13-8 ⁱ Pr * n * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ 11-14-1 ^t bu N n n Et H F H OH H H NH ₂ 11-14-2 ^t bu N n CH ₃ Et H F H OH H H NH ₂ 11-14-3 ^t bu N n CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ 11-14-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ 11-14-5 ^t bu n n CH ₂ Ph Et H F H OH H H NH ₂ 11-14-6 ^t bu n n CH ₂ -indol-3-yl Et H F H OH H H NH ₂ 11-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ 11-14-8 ^t bu * n * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-15-1 Ph H H H Et H F H OH H H NH ₂ VII-15-2 Ph H H CH ₃ Et H F H OH H H NH ₂ VII-15-3 Ph H H CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-15-5 Ph H H CH ₂ Ph Et H F H OH H H NH ₂ VII-15-6 Ph H H CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-15-8 Ph * H * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-16-1 p-me-ph H H H Et H F H OH H H NH ₂ VII-16-2 p-me-ph H H CH ₃ Et H F H OH H H NH ₂ VII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-16-5 p-me-ph H H CH ₂ Ph Et H F H OH H H NH ₂ VII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-16-8 p-me-ph * H * Et H F H OH H H NH ₂

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-17-1 p-f-ph H H H Et H F H OH H H NH ₂ VII-17-2 p-f-ph H H CH ₃ Et H F H OH H H NH ₂ VII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-17-5 p-f-ph H H CH ₂ Ph Et H F H OH H H NH ₂ VII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-17-8 p-f-ph H * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-18-1 p-Cl-Ph H H H Et H F H OH H H NH ₂ VII-18-2 p-Cl-Ph H H CH ₃ Et H F H OH H H NH ₂ VII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-18-5 p-Cl-Ph H H CH ₂ Ph Et H F H OH H H NH ₂ VII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-18-8 p-Cl-Ph H * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-19-1 p-Br-Ph H H H Et H F H OH H H NH ₂ VII-19-2 p-Br-Ph H H CH ₃ Et H F H OH H H NH ₂ VII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-19-5 p-Br-Ph H H CH ₂ Ph Et H F H OH H H NH ₂ VII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-19-8 p-Br-Ph * H Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-20-1 p-1-ph N N n Et H F H OH H H NH ₂ VII-20-2 p-1-ph N N CH ₃ Et H F H OH H H NH ₂ VII-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et H F H OH H H NH ₂ VII-20-5 p-1-ph N N CH ₂ Ph Et H F H OH H H NH ₂ VII-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H F H OH H H NH ₂ VII-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H F H OH H H NH ₂ VII-20-8 p-1-ph * n * Et H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-21-1 CH ₃ N n n ⁱ Pr N F N IT N N NH ₂ VII-21-2 CH ₃ N n CH ₃ ⁱ Pr N F N IT N N NH ₂ VII-21-3 CH ₃ n n CH (CH ₃ ) ₂ ⁱ Pr N F N IT N n NH ₂ VII-21-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F N IT N n NH ₂ VII-21-5 CH ₃ n n CH ₂ Ph ⁱ Pr N F N IT N n NH ₂ VII-21-6 CH ₃ n n CH ₂ -indol-3-yl ⁱ Pr N F N IT N n NH ₂ VII-21-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F N IT N n NH ₂ VII-21-8 CH ₃ * n ⁱ Pr N F N IT N n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-22. No. R R Rja Rib R R R X Y R R Ry VII-22-1 Et H H H ⁱ Pr H F H OH H H NH ₂ VII-22-2 Et H H CH ₃ ⁱ Pr H F H OH H H NH ₂ VII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-22-5 Et H H CH ₂ Ph ⁱ Pr H F H OH H H NH ₂ VII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H NH ₂ VII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H NH ₂ VII-22-8 Et * H * ⁱ Pr H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-23-1 ⁱ Pr N N n ⁱ Pr N F n IT n n NH ₂ VII-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N F n it n n NH ₂ VII-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr N F n it n n NH ₂ VII-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F n it n n NH ₂ VII-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr N F n it n n NH ₂ VII-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr N F n it n n NH ₂ VII-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it n n NH ₂ VII-23-8 ⁱ Pr * n * ⁱ Pr n F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-24-1 ^t bu N n n ⁱ Pr N F n IT n n NH ₂ VII-24-2 ^t bu N n CH ₃ ⁱ Pr N F n IT n n NH ₂ VII-24-3 ^t bu n n CH (CH ₃ ) ₂ ⁱ Pr n F n it n n NH ₂ VII-24-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F n it n n NH ₂ VII-24-5 ^t bu n n CH ₂ Ph ⁱ Pr n F n it n n NH ₂ VII-24-6 ^t bu n n CH ₂ -indol-3-yl ⁱ Pr n F n it n n NH ₂ VII-24-7 ^t bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it n n NH ₂ VII-24-8 ^t bu * n * ⁱ Pr n F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-25-1 Ph H H H ⁱ Pr H F H OH H H NH ₂ VII-25-2 Ph H H CH ₃ ⁱ Pr H F H OH H H NH ₂ VII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-25-5 Ph H H CH ₂ Ph ⁱ Pr H F H OH H H NH ₂ VII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H NH ₂ VII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H NH ₂ VII-25-8 Ph * H * ⁱ Pr H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-26-1 p-me-ph H H H ⁱ Pr H F H OH H H NH ₂ VII-26-2 p-me-ph H H CH ₃ ⁱ Pr H F H OH H H NH ₂ VII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F H OH H H NH ₂ VII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H NH ₂ VII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H NH ₂ VII-26-8 p-me-ph * H * ⁱ Pr H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-27-1 p-f-ph H H H ⁱ Pr H F H OH H H NH ₂ VH-27-2 p-f-ph H H CH ₃ ⁱ Pr H F H OH H H NH ₂ VII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F H OH H H NH ₂ VII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H NH ₂ VII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H NH ₂ VII-27-8 p-f-ph * H * ⁱ Pr H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-28-1 p-Cl-Ph H H H ⁱ Pr H F H OH H H NH ₂ VII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F H OH H H NH ₂ VII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F H OH H H NH ₂ VII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H NH ₂ VII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H NH ₂ VII-28-8 p-Cl-Ph * H * ⁱ Pr H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-29-1 p-Br-Ph H H H ⁱ Pr H F H OH H H NH ₂ VII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F H OH H H NH ₂ VII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH H H NH ₂ VII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F H OH H H NH ₂ VII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH H H NH ₂ VII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH H H NH ₂ VII-29-8 p-Br-Ph * H * ⁱ Pr H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-30-1 p-1-ph N n n ⁱ Pr N F n IT n n NH ₂ VII-30-2 p-1-ph N n CH ₃ ⁱ Pr N F n it n n NH ₂ VII-30-3 p-1-ph n n CH (CH ₃ ) ₂ ⁱ Pr N F n it n n NH ₂ VII-30-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F n it n n NH ₂ VII-30-5 p-1-ph n n CH ₂ Ph ⁱ Pr N F n it n n NH ₂ VII-30-6 p-1-ph n n CH ₂ -indol-3-yl ⁱ Pr N F n it n n NH ₂ VII-30-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F n it n n NH ₂ VII-30-8 p-1-ph * n ⁱ Pr N F n it n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-31-1 CH ₃ N n n ⁿ Bu H F H OH H H NH ₂ VII-31-2 CH ₃ N n CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-31-3 CH ₃ n n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-31-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-31-5 CH ₃ n n CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-31-6 CH ₃ n n CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-31-8 CH ₃ * n * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-32-1 Et H H H ⁿ Bu H F H OH H H NH ₂ VII-32-2 Et H H CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-32-5 Et H H CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-32-8 Et * H * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-33-1 ⁱ Pr N n n ⁿ Bu H F H OH H H NH ₂ VII-33-2 ⁱ Pr N n CH ₃ ⁿ Bu H F H OH H H NH ₂ VTI-33-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-33-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-33-5 ⁱ Pr n n CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-33-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-33-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-33-8 ⁱ Pr * n * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-34-1 ^t bu N N n ⁿ Bu N F N IT N n NH ₂ VII-34-2 ^t bu N N CH ₃ ⁿ Bu N F N IT N n NH ₂ VII-34-3 ^t bu N N CH (CH ₃ ) ₂ ⁿ Bu N F N IT N n NH ₂ VII-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N F N IT N n NH ₂ VII-34-5 ^t bu N n CH ₂ Ph ⁿ Bu N F N IT N n NH ₂ VII-34-6 ^t bu N n CH ₂ -indol-3-yl ⁿ Bu N F N IT N n NH ₂ VII-34-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N F N IT n n NH ₂ VII-34-8 ^t bu * n * ⁿ Bu N F N IT n n NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-35-1 Ph H H H ⁿ Bu H F H OH H H NH ₂ VII-35-2 Ph H H CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-35-5 Ph H H CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-35-8 Ph * H * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-36-1 p-me-ph H H H ⁿ Bu H F H OH H H NH ₂ VII-36-2 p-me-ph H H CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-36-8 p-me-ph * H ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VH-37-1 p-f-ph H- H H ⁿ Bu H F H OH H H NH ₂ VII-37-2 p-f-ph H H CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-37-8 p-f-ph * H * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-38-1 p-Cl-Ph H H H ⁿ Bu H F H OH H H NH ₂ VII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F H OH H H NH ₂ VH-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-38-8 p-Cl-Ph H * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-39-1 p-Br-Ph H H H ⁿ Bu H F H OH H H NH ₂ VII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-39-8 p-Br-Ph * H * ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-40-1 p-1-ph N N n ⁿ Bu H F H OH H H NH ₂ VII-40-2 p-1-ph N N CH ₃ ⁿ Bu H F H OH H H NH ₂ VII-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH H H NH ₂ VII-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H F H OH H H NH ₂ VII-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H F H OH H H NH ₂ VII-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH H H NH ₂ VII-40-8 p-1-ph * n ⁿ Bu H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-41-1 CH ₃ N n n Bz H F H OH H H NH ₂ VII-41-2 CH ₃ N n CH ₃ Bz H F H OH H H NH ₂ VII-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-41-5 CH ₃ n n CH ₂ Ph Bz H F H OH H H NH ₂ VII-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-41-8 CH ₃ * n * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-42-1 Et H H H Bz H F H OH H H NH ₂ VII-42-2 Et H H CH ₃ Bz H F H OH H H NH ₂ VII-42-3 Et H H CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-42-5 Et H H CH ₂ Ph Bz H F H OH H H NH ₂ VII-42-6 Et H H CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-42-8 Et H * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-43-1 ⁱ Pr N n n Bz H F H OH H H NH ₂ VII-43-2 ⁱ Pr N n CH ₃ Bz H F H OH H H NH ₂ VII-43-3 ⁱ Pr n n CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-43-5 ⁱ Pr n n CH ₂ Ph Bz H F H OH H H NH ₂ VII-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-43-8 ⁱ Pr * n * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-44-1 ^t bu N N n Bz H F H OH H H NH ₂ VH-44-2 ^t bu N N CH ₃ Bz H F H OH H H NH ₂ VII-44-3 ^t bu N N CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-44-5 ^t bu N n CH ₂ Ph Bz H F H OH H H NH ₂ VII-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-44-8 ^t bu * n * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-45-1 Ph H H H Bz H F H OH H H NH ₂ VII-45-2 Ph H H CH ₃ Bz H F H OH H H NH ₂ VII-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-45-5 Ph H H CH ₂ Ph Bz H F H OH H H NH ₂ VII-45-6 Ph H H CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-45-8 Ph * H Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-46-1 p-me-ph H H H Bz H F H OH H H NH ₂ VII-46-2 p-me-ph H H CH ₃ Bz H F H OH H H NH ₂ VII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-46-5 p-me-ph H H CH ₂ Ph Bz H F H OH H H NH ₂ VII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-46-8 p-me-ph H Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-47-1 p-f-ph H H H Bz H F H OH H H NH ₂ VII-47-2 p-f-ph H H CH ₃ Bz H F H OH H H NH ₂ VII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-47-5 p-f-ph H H CH ₂ Ph Bz H F H OH H H NH ₂ VII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-47-8 p-f-ph * H * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-48-1 p-Cl-Ph H H H Bz H F H OH H H NH ₂ VII-48-2 p-Cl-Ph H H CH ₃ Bz H F H OH H H NH ₂ VII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F H OH H H NH ₂ VII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-48-8 p-Cl-Ph * H * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-49-1 p-Br-Ph H H H Bz H F H OH H H NH ₂ VII-49-2 p-Br-Ph H H CH ₃ Bz H F H OH H H NH ₂ VII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-49-5 p-Br-Ph H H CH ₂ Ph Bz H F H OH H H NH ₂ VII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-49-8 p-Br-Ph * H * Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ R ⁹ VII-50-1 p-1-ph N N N Bz H F H OH H H NH ₂ VH-50-2 p-1-ph N N CH ₃ Bz H F H OH H H NH ₂ VII-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH H H NH ₂ VII-50-5 p-1-ph N n CH ₂ Ph Bz H F H OH H H NH ₂ VII-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H F H OH H H NH ₂ VII-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H F H OH H H NH ₂ VII-50-8 p-1-ph * n Bz H F H OH H H NH ₂ * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-1-1 CH ₃ N N N CH ₃ N CH ₃ it it n n VIII-1-2 CH ₃ N N CH ₃ CH ₃ N CH ₃ it it n n VIIM-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n VIII-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n VIII-1-5 CH ₃ N n CH ₂ Ph CH ₃ N CH ₃ it it n n VIII-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N CH ₃ it it n n VHI-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ it it n n VHI-1-8 CH ₃ * n CH ₃ N CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-2-1 Et H H H CH ₃ H CH ₃ it it n n VIII-2-2 Et H H CH ₃ CH ₃ H CH ₃ it it n n VIII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ it it n n VIII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ it it n n VIII-2-5 Et H H CH ₂ Ph CH ₃ H CH ₃ it it n n VIII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H CH ₃ it it n n VIII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ it it n n VIII-2-8 Et * H * CH ₃ H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-3-1 ⁱ Pr H H H CH ₃ n CH ₃ it it n n VHI-3-2 ⁱ Pr H H CH ₃ CH ₃ n CH ₃ it it n n VHI-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ it it n n VIII-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ it it n n VIII-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ n CH ₃ it it n n VIII-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ n CH ₃ it it n n VIII-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ it it n n VIII-3-8 ⁱ Pr * H CH ₃ n CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-4-1 ^t bu N N n CH ₃ N CH ₃ IT IT n n VIII-4-2 ^t bu N N CH ₃ CH ₃ N CH ₃ IT it n n VIII-4-3 ^t bu N N CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT it n n VIII-4-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ IT it n n VIII-4-5 ^t bu N n CH ₂ Ph CH ₃ N CH ₃ IT it n n VIII-4-6 ^t bu N n CH ₂ -indol-3-yl CH ₃ N CH ₃ it it n n VIII-4-7 ^t bu n n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ it it n n VIII-4-8 ^t bu * n * CH ₃ N CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-5-1 Ph H H H CH ₃ H CH ₃ OH OH H H VIII-5-2 Ph H H CH ₃ CH ₃ H CH ₃ OH OH H H VIII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-5-5 Ph H H CH ₂ Ph CH ₃ H CH ₃ OH OH H H VIII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ OH OH H H VIII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ OH OH H H VIII-5-8 Ph * H * CH ₃ H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-6-1 p-me-ph H H H CH ₃ H CH ₃ OH OH H H VHI-6-2 p-me-ph H H CH ₃ CH ₃ H CH ₃ OH OH H H VIII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-6-5 p-me-ph H H CH ₂ Ph CH ₃ H CH ₃ OH OH H H VIII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ OH OH H H VIII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ OH OH H H VIII-6-8 p-me-ph * H * CH ₃ H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-7-1 p-f-ph H H H CH ₃ H CH ₃ OH OH H H VIII-7-2 p-f-ph H H CH ₃ CH ₃ H CH ₃ OH OH H H VIII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-7-6 p-f-ph H H CH ₂ Ph CH ₃ H CH ₃ OH OH H H VIII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ OH OH H H VIII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ OH OH H H VIII-7-20 p-f-ph * H * CH ₃ H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIH-8-1 p-Cl-Ph H H H CH ₃ H CH ₃ OH OH H H VIII-8-2 p-Cl-Ph H H CH ₃ CH ₃ H CH ₃ OH OH H H VIII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ H CH ₃ OH OH H H VIII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ OH OH H H VIII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ OH OH H H VIII-8-8 p-Cl-Ph * H * CH ₃ H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-9-1 p-Br-Ph H H H CH ₃ H CH ₃ OH OH H H VIII-9-2 p-Br-Ph H H CH ₃ CH ₃ H CH ₃ OH OH H H VIII-9-3 r-br-ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ OH OH H H VIII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ H CH ₃ OH OH H H VIII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ OH OH H H VIII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ OH OH H H VIII-9-20 p-Br-Ph * H * CH ₃ H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-10-1 p-1-ph N N n CH ₃ n CH ₃ it it n n VIII-10-2 p-1-ph N N sn3 CH ₃ n CH ₃ it it n n VIII-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N CH ₃ it it n n VIII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N sun ₃ it it n n VIII-10-5 p-1-ph N n CH ₂ Ph CH ₃ N sun ₃ it it n n VIII-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ N sun ₃ it it n n VIII-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ N sun ₃ it it n n VIII-10-8 p-1-ph * n * sun ₃ N sun ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-11-1 CH ₃ N H H Et H CH ₃ IT IT n n VIII-11-2 CH ₃ N N CH ₃ Et H CH ₃ IT it n n VIII-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H CH ₃ IT it n n VIII-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ IT it n n VIII-11-5 CH ₃ N n CH ₂ Ph Et H CH ₃ it it n n VIII-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H CH ₃ it it n n VIII-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ it it n n VIII-11-8 CH ₃ * n * Et H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-12-1 Et H H H Et H CH ₃ IT it n n VIII-12-2 Et H H CH ₃ Et H CH ₃ it it n n VIII-12-3 Et H H CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIII-12-5 Et H H CH ₂ Ph Et H CH ₃ it it n n VIII-12-6 Et H H CHg-indol-3-yl Et H CH ₃ it it n n VIII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ it it n n VIII-12-8 Et * H * Et H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-13-1 ⁱ Pr n N n Et H CH ₃ IT it n n VIII-13-2 ⁱ Pr N N CH ₃ Et H CH ₃ IT it n n VIII-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIII-13-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIII-13-5 ⁱ Pr N N CH ₂ Ph Et H CH ₃ it it n n VIII-13-6 ⁱ Pr N N CH ₂ -indol-3-yl Et H CH ₃ it it n n VIII-13-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Et H CH ₃ it it n n VIII-13-8 ⁱ Pr * n * Et H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ V1II-14-1 ^t bu N N n Et H CH ₃ OH OH H H VIII-14-2 ^t bu N N CH ₃ Et H CH ₃ OH OH H H VIII-14-3 ^t bu N N CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-14-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-14-5 ^t bu N N CH ₂ Ph Et H CH ₃ OH OH H H VIII-14-6 ^t bu n n CH ₂ -indol-3-yl Et H CH ₃ OH OH H H VIII-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H CH ₃ OH OH H H VIII-14-8 ^t bu * n * Et H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-15-1 Ph H H H Et H CH ₃ OH OH H H VIII-15-2 Ph H H CH ₃ Et H CH ₃ OH OH H H VHI-15-3 Ph H H CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-15-5 Ph H H CH ₂ Ph Et H CH ₃ OH OH H H VIII-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ OH OH H H VIII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ OH OH H H VHI-15-8 Ph * H * Et H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-16-1 p-me-ph H H H Et H CH ₃ OH OH H H VIII-16-2 p-me-ph H H CH ₃ Et H CH ₃ OH OH H H VIII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-16-5 p-me-ph H H CH ₂ Ph Et H CH ₃ OH OH H H VIII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ OH OH H H VIII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ OH OH H H VIII-16-8 p-me-ph * H * Et H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-17-1 p-f-ph H H H Et H CH ₃ IT IT n n VIII-17-2 p-f-ph H H CH ₃ Et H CH ₃ IT IT n n VHI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ IT it n n VIII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ IT it n n VIII-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ IT it n n VIII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ it it n n VHI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ it it n n VIII-17-8 p-f-ph * H * Et H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-18-1 p-Cl-Ph H H H Et H CH ₃ IT it n n VIII-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ IT it n n VIII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIII-18-5 p-Cl-Ph H H CH ₂ Ph Et H CH ₃ it it n n VIII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H CH ₃ it it n n VIII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ it it n n VIII-18-8 p-Cl-Ph * H * Et H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-19-1 p-Br-Ph H N n Et H CH ₃ IT it n n VIII-19-2 p-Br-Ph H n CH ₃ Et H CH ₃ IT it n n VIII-19-3 r-vg-ph N n CH (CH ₃ ) ₂ Et H CH ₃ IT it n n VIII-19-4 p-Br-Ph N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ it it n n VIIM9-5 p-Br-Ph N n CH ₂ Ph Et H CH ₃ it it n n VHI-19-6 p-Br-Ph N n CH ₂ -indol-3-yl Et H CH ₃ it it n n VIII-19-7 p-Br-Ph N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ it it n n VIII-19-8 p-Br-Ph * n * Et H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-20-1 p-1-ph N N N Et H CH ₃ OH OH H H VIII-20-2 p-1-ph N N CH ₃ Et H CH ₃ OH OH H H VIII-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ OH OH H H VIII-20-5 p-1-ph N N CH ₂ Ph Et H CH ₃ OH OH H H VIII-20-6 p-1-ph N N CH ₂ -indol-3-yl Et H CH ₃ OH OH H H VIII-20-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Et H CH ₃ OH OH H H VIII-20-8 p-1-ph * N * Et H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-21-1 CH ₃ N N n ⁱ Pr N CH ₃ IT it n n VIII-21-2 CH ₃ N N CH ₃ ⁱ Pr N CH ₃ IT it n n VIII-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ it it n n VHI-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ it it n n VIII-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr n CH ₃ it it n n VIII-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ it it n n VIII-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ it it n n VIII-21-8 CH ₃ * n * ⁱ Pr n CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-22-1 Et H H H ⁱ Pr H CH ₃ IT it n n VIII-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ it it n n VHI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ it it n n VIII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ it it n n VIII-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ it it n n VIII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ it it n n VIII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ it it n n VIII-22-8 Et * H * ⁱ Pr H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-23-1 ⁱ Pr N n n ⁱ Pr N CH ₃ IT it n n VIII-23-2 ⁱ Pr N n CH ₃ ⁱ Pr N CH ₃ IT it n n VIII-23-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ IT it n n VIII-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ IT it n n VIII-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr n CH ₃ IT it n n VHI-23-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ IT it n n VIII-23-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ it it n n VIII-23-8 ⁱ Pr * n * ⁱ Pr n CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-24-1 ^t bu N N n ⁱ Pr N CH ₃ it it n n VIII-24-2 ^t bu N N CH ₃ ⁱ Pr N CH ₃ IT it n n VIII-24-3 ^t bu N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ IT it n n VIII-24-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ IT it n n VHI-24-5 ^t bu N n CH ₂ Ph ⁱ Pr n CH ₃ it it n n VIII-24-6 ^t bu N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ it it n n VIII-24-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ it it n n VIII-24-8 ^t bu * n * ⁱ Pr n CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-25-1 Ph H H H ⁱ Pr H CH ₃ IT IT n n VIII-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ IT it n n VIII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT it n n VIII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT it n n VIII-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ IT it n n VIII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ it it n n VIII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ it it n n VIII-25-8 Ph * H * ⁱ Pr H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VTII-26-1 p-me-ph H H H ⁱ Pr H CH ₃ IT IT n n VIII-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ IT it n n VIII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT it n n VIII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT it n n VHI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ it it n n VIII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ it it n n VIII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ it it n n VIII-26-8 p-me-ph * H * ⁱ Pr H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-27-1 p-f-ph H H H ⁱ Pr H CH ₃ IT it n n VIII-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ IT it n n VIII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ IT it n n VIII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ it it n n VIII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ it it n n VIII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ it it n n VIII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ it it n n VIII-27-8 p-f-ph * H * ⁱ Pr H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-28-1 p-Cl-Ph H H H ^t Pr H CH ₃ IT IT n n VIII-28-2 p-Cl-Ph H H CH ₃ ^t Pr H CH ₃ IT IT n n VIII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ * Pr H CH ₃ IT IT n n VIII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ^t Pr H CH ₃ IT it n n VIII-28-5 p-Cl-Ph H H CH ₂ Ph * Pr H CH ₃ IT it n n VIII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl * Pr H CH ₃ it it n n VIII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ^t Pr H CH ₃ it it n n VIII-28-8 p-Cl-Ph * H * * Pr H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ IT it n n VIII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ it it n n VIII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ it it n n VIII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ it it n n VIII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ it it n n VIII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ it it n n VIII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ it it n n VIII-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-30-1 p-1-ph N n n ⁱ Pr N CH ₃ it it n n VHI-30-2 p-1-ph N n CH ₃ ⁱ Pr N CH ₃ it it n n VIII-30-3 p-1-ph n n CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ it it n n VIII-30-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ it it n n VIII-30-5 p-1-ph n n CH ₂ Ph ⁱ Pr N CH ₃ it it n n VIII-30-6 p-1-ph n n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ it it n n VIII-30-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ it it n n VIII-30-8 p-1-ph * n * ⁱ Pr n CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-31-1 CH ₃ N n n ⁿ Bu H CH ₃ IT it n n VIII-31-2 CH ₃ N n CH ₃ ⁿ Bu H CH ₃ IT it n n VIII-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VIII-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-31-5 CH ₃ n n CH ₂ Ph ⁿ Bu H CH ₃ it it n n VIII-31-6 CH ₃ n n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n VIII-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VIII-31-8 CH ₃ * n * ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-32-1 Et H H H ⁿ Bu H CH ₃ OH OH H H VIII-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ OH OH H H VIII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ OH OH H H VIII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ OH OH H H VIII-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ OH OH H H VIII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ OH OH H H VIII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ OH OH H H VIII-32-8 Et * H * ⁿ Bu H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-33-1 ⁱ Pr N n n ⁿ Bu H CH ₃ OH OH H H VIII-33-2 ⁱ Pr N n CH ₃ ⁿ Bu H CH ₃ OH OH H H VIII-33-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ OH OH H H VIII-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ OH OH H H VIII-33-5 ⁱ Pr n n CH ₂ Ph ⁿ Bu H CH ₃ OH OH H H VIII-33-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ OH OH H H VIII-33-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ OH OH H H VIII-33-8 ⁱ Pr * n * ⁿ Bu H CH ₃ OH OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-34-1 ^t bu N N n ⁿ Bu N CH ₃ IT it n n VIII-34-2 ^t bu N N CH ₃ ⁿ Bu n CH ₃ IT it n n VIII-34-3 ^t bu N N CH (CH ₃ ) ₂ ⁿ Bu n CH ₃ it it n n VIII-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu n CH ₃ it it n n VIII-34-5 ^t bu N n CH ₂ Ph ⁿ Bu n CH ₃ it it n n VIII-34-6 ^t bu N n CH ₂ -indol-3-yl ⁿ Bu n CH ₃ it it n n VIII-34-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu n CH ₃ it it n n VIII-34-8 ^t bu * n * ⁿ Bu n CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-35-1 Ph H H H ⁿ Bu H CH ₃ IT it n n VIII-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ IT it n n VIII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n VIII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n VHI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VIII-35-8 Ph * H * ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-36-1 p-me-ph H H H ⁿ Bu H CH ₃ IT it n n VHI-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ IT it n n VIII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VHI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VTII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n VIII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n VIII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VHI-36-8 p-me-ph * H * ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-37-1 p-f-ph H H H ⁿ Bu H CH ₃ IT IT n n VIII-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ IT it n n VIII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VIII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VHI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ IT it n n VIII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ IT it n n VIII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VIII-37-8 p-f-ph * H ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ it it n n VIII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ it it n n VIII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n VIII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n VIII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VTII-38-8 p-Cl-Ph * H * ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ it it n n VIII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ it it n n VIII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ it it n n VIII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ it it n n VIII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n VIII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VIII-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-40-1 p-1-ph n n n ⁿ Bu H CH ₃ IT IT n n VIII-40-2 p-1-ph n n CH ₃ ⁿ Bu H CH ₃ IT it n n VIII-40-3 p-1-ph n n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VIII-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ IT it n n VHI-40-5 p-1-ph n n CH ₂ Ph ⁿ Bu H SI IT it n n VIII-40-6 p-1-ph n n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ it it n n VIII-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ it it n n VIII-40-8 p-1-ph * n * ⁿ Bu H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-41-1 CH ₃ N n n Bz H CH ₃ IT IT n n VHI-41-2 CH ₃ N n CH ₃ Bz H CH ₃ IT it n n VIII-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n VIII-41-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n VIII-41-5 CH ₃ N n CH ₂ Ph Bz H CH ₃ it it n n VIII-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H CH ₃ it it n n VHI-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-41-8 CH ₃ * n * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-42-1 Et H H H Bz H CH ₃ IT IT n n VIII-42-2 Et H H CH ₃ Bz H CH ₃ IT it n n VIII-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n VIII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n VIII-42-5 Et H H CH ₂ Ph Bz H CH ₃ IT it n n VIII-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-42-8 Et * H * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-43-1 ⁱ Pr N N n Bz H CH ₃ it it n n VIII-43-2 ⁱ Pr N N CH ₃ Bz H CH ₃ it it n n VIII-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-43-5 ⁱ Pr N n CH ₂ Ph Bz H CH ₃ it it n n VIII-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-43-8 ⁱ Pr * n * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-44-1 ^t bu N N n Bz H CH ₃ IT it n n VIII-44-2 ^t bu N N CH ₃ Bz H CH ₃ it it n n VIII-44-3 ^t bu N N CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-44-5 ^t bu N n CH ₂ Ph Bz H CH ₃ it it n n VIII-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-44-8 ^t bu n * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-45-1 Ph H H H Bz H CH ₃ IT it n n VIII-45-2 Ph H H CH ₃ Bz H CH ₃ IT it n n V1II-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ IT it n n VIII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-45-5 Ph H H CH ₂ Ph Bz H CH ₃ it it n n VIII-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-45-8 Ph * H * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VHI-46-1 p-me-ph H H H Bz H CH ₃ it it n n VIII-46-2 p-me-ph H H CH ₃ Bz H CH ₃ it it n n VHI-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ it it n n VIII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-46-8 p-me-ph * H * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-47-1 p-f-ph H H H Bz H CH ₃ it it n n VIII-47-2 p-f-ph H H CH ₃ Bz H CH ₃ it it n n VIII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ it it n n VIII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-47-8 p-f-ph * H * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-48-1 p-Cl-Ph H H H Bz H CH ₃ it it n n VIII-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ it it n n VIII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ it it n n VIII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-48-8 p-Cl-Ph * H * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table VIII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-49-1 p-Br-Ph H H H Bz H CH ₃ IT it n n VIII-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ it it n n VIII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ it it n n VIII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-49-8 p-Br-Ph * H * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table VIII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ VIII-50-1 p-1-ph N N n Bz H CH ₃ IT it n n VIII-50-2 p-1-ph N N CH ₃ Bz H CH ₃ it it n n VIII-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-50-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ it it n n VIII-50-5 p-1-ph N N CH ₂ Ph Bz H CH ₃ it it n n VIII-50-6 p-1-ph N N CH ₂ -indol-3-yl Bz H CH ₃ it it n n VIII-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ it it n n VIII-50-8 p-1-ph * n * Bz H CH ₃ it it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-1-1 CH ₃ N n n CH ₃ N CH ₃ F IT N N IX-1-2 CH ₃ N n CH ₃ CH ₃ N CH ₃ F IT N N IX-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N IX-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N IX-1-5 CH ₃ n n CH ₂ Ph CH ₃ N CH ₃ F IT N N IX-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT N N IX-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT N N IX-1-8 CH ₃ * n * CH ₃ N CH ₃ F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-2-1 Et H H H CH ₃ N CH ₃ F IT N N IX-2-2 Et H H CH ₃ CH ₃ N CH ₃ F IT N N IX-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N IX-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n N IX-2-5 Et H H CH ₂ Ph CH ₃ N CH ₃ F IT n N IX-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT n n IX-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT n n IX-2-8 Et * H * CH ₃ N CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-3-1 ⁱ Pr n N n CH ₃ N CH ₃ F IT N N IX-3-2 ⁱ Pr n N CH ₃ CH ₃ N CH ₃ F IT N N IX-3-3 ⁱ Pr n N CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n N IX-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n N IX-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ n CH ₃ F IT n n IX-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT n n IX-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT n n IX-3-8 ⁱ Pr * n * CH ₃ n CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-4-1 ^t bu n n n CH ₃ N CH ₃ F IT N n IX-4-2 ^t bu n n CH ₃ CH ₃ N CH ₃ F IT N n IX-4-3 ^t bu n n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n n IX-4-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n n IX-4-5 ^t bu n n CH ₂ Ph CH ₃ N CH ₃ F IT n n IX-4-6 ^t bu n n CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT n n IX-4-7 ^t bu n n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT n n IX-4-8 ^t bu * N * CH ₃ n CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-5-1 Ph H H H CH ₃ N CH ₃ F IT N N IX-5-2 Ph H H CH ₃ CH ₃ N CH ₃ F IT N N IX-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N IX-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N N IX-5-5 Ph H H CH ₂ Ph CH ₃ N CH ₃ F IT N N IX-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT N N IX-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT N n IX-5-8 Ph H * CH ₃ N CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-6-1 p-me-ph H H H CH ₃ N CH ₃ F IT N n IX-6-2 p-me-ph H H CH ₃ CH ₃ N CH ₃ F IT N n IX-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n IX-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n IX-6-S p-me-ph H H CH ₂ Ph CH ₃ n CH ₃ F IT n n IX-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT n n IX-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT n n IX-6-8 p-me-ph * H * CH ₃ n CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-7-1 p-f-ph H H H CH ₃ N CH ₃ F IT n n IX-7-2 p-f-ph H H CH ₃ CH ₃ N CH ₃ F IT n n IX-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n n IX-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n n IX-7-6 p-f-ph H H CH ₂ Ph CH ₃ N CH ₃ F IT n n IX-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT n n IX-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F it n n IX-7-20 p-f-ph * H * CH ₃ N CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-8-1 p-Cl-Ph H H H CH ₃ N CH ₃ F IT n n IX-8-2 p-Cl-Ph H H CH ₃ CH ₃ N CH ₃ F IT n n IX-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n n IX-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT n n IX-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N CH ₃ F IT n n IX-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT n n IX-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT n n IX-8-8 p-Cl-Ph * H * CH ₃ N CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-9-1 p-Br-Ph H H H CH ₃ N CH ₃ F IT N n IX-9-2 p-Br-Ph H H CH ₃ CH ₃ N CH ₃ F IT N n IX-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N n IX-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT N n IX-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N CH ₃ F IT N n IX-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT N n IX-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT N n IX-9-20 p-Br-Ph * H * CH ₃ N CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-10-1 p-1-ph n n n CH ₃ n CH ₃ F IT N N IX-10-2 p-1-ph n n CH ₃ CH ₃ n CH ₃ F IT N N IX-10-3 p-1-ph n n CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n IX-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT n n IX-10-5 p-1-ph N n CH ₂ Ph CH ₃ n CH ₃ F IT n n IX-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ n CH ₃ F it n n IX-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F it n n IX-10-8 p-1-ph * n * CH ₃ n CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX - 11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-11-1 CH ₃ N N n Et H CH ₃ F IT N N IX-11-2 CH ₃ N N CH ₃ Et H CH ₃ F IT N N IX-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H CH ₃ F IT N N IX-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N N IX-11-5 CH ₃ N n CH ₂ Ph Et H CH ₃ F IT N n IX-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H CH ₃ F IT N n IX-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N n IX-11-8 CH ₃ * n * Et H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-12-1 Et H H H Et H CH ₃ F IT N n IX-12-2 Et H H CH ₃ Et H CH ₃ F IT N N IX-12-3 Et H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N N IX-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N N IX-12-5 Et H H CH ₂ Ph Et H CH ₃ F IT N N IX-12-6 Et H H CH ₂ -indol-3-yl Et H CH ₃ F IT n N IX-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-12-8 Et * H * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-13-1 ⁱ Pr N N n Et H CH ₃ F IT N n IX-13-2 ⁱ Pr N N CH ₃ Et H CH ₃ F IT n n IX-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H CH ₃ F IT n n IX-13-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n n IX-13-5 ⁱ Pr N N CH ₂ Ph Et H CH ₃ F IT n n IX-13-6 ⁱ Pr N N CH ₂ -indol-3-yl Et H CH ₃ F IT n n IX-13-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-13-8 ⁱ Pr * N * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-14-1 ^t bu N n n Et H CH ₃ F IT N n IX-14-2 ^t bu N n CH ₃ Et H CH ₃ F IT N n IX-14-3 ^t bu N n CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-14-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-14-5 ^t bu N n CH ₂ Ph Et H CH ₃ F IT N n IX-14-6 ^t bu n n CH ₂ -indol-3-yl Et H CH ₃ F IT N n IX-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-14-8 ^t bu * n * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-15-1 Ph H H H Et H CH ₃ F IT N n IX-15-2 Ph H H CH ₃ Et H CH ₃ F IT N n IX-15-3 Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT n n IX-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n n IX-15-5 Ph H H CH ₂ Ph Et H CH ₃ F IT n n IX-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n IX-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-15-8 Ph * H * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-16-1 p-me-ph H H H Et H CH ₃ F IT N n IX-16-2 p-me-ph H H CH ₃ Et H CH ₃ F IT N n IX-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT n n IX-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT n n IX-16-5 p-me-ph H H CH ₂ Ph Et H CH ₃ F IT n n IX-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n IX-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-16-8 p-me-ph * H * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-17-1 p-f-ph H H H Et H CH ₃ F IT N n IX-17-2 p-f-ph H H CH ₃ Et H CH ₃ F IT N n IX-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ F IT n n IX-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n IX-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-17-8 p-f-ph * H * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-18-1 p-Cl-Ph H H H Et H CH ₃ F IT N N IX-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ F IT N N IX-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-18-5 p-Cl-Ph H H CH ₂ Ph Et H CH ₃ F IT N n IX-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT N n IX-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N n IX-18-8 p-Cl-Ph * H * Et H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-19-1 p-Br-Ph H H H Et H CH ₃ F IT N N IX-19-2 p-Br-Ph H H CH ₃ Et H CH ₃ F IT N n IX-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N n IX-19-5 p-Br-Ph H H CH ₂ Ph Et H CH ₃ F IT N n IX-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT n n IX-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT n n IX-19-8 p-Br-Ph * H * Et H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-20-1 p-1-ph N n n Et H CH ₃ F IT N N IX-20-2 p-1-ph N n CH ₃ Et H CH ₃ F IT N N IX-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et H CH ₃ F IT N N IX-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT N N IX-20-5 p-1-ph N n CH ₂ Ph Et H CH ₃ F IT N N IX-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H CH ₃ F IT N N IX-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT N N IX-20-8 p-1-ph * n * Et H CH ₃ F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-21-1 CH ₃ N N n ⁱ Pr N CH ₃ F IT N n IX-21-2 CH ₃ N N CH ₃ ⁱ Pr N CH ₃ F IT N n IX-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT n n IX-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT n n IX-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr n CH ₃ F IT n n IX-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT n n IX-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT n n IX-21-8 CH ₃ * n * ⁱ Pr n CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-22-1 Et H H H ⁱ Pr H CH ₃ F IT N n IX-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ F IT N n IX-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N N IX-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N N IX-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ F IT n N IX-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n N IX-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n IX-22-8 Et * H * ⁱ Pr H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-23-1 ⁱ Pr N N N ⁱ Pr N CH ₃ F IT N N IX-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N CH ₃ F IT N N IX-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N n IX-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N n IX-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr N CH ₃ F IT N n IX-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT N n IX-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT N n IX-23-8 ⁱ Pr * N * ⁱ Pr N CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-24-1 ^t bu N N n ⁱ Pr N CH ₃ F IT N N IX-24-2 ^t bu N N CH ₃ ⁱ Pr N CH ₃ F IT N N IX-24-3 ^t bu N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N IX-24-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N IX-24-5 ^t bu N N CH ₂ Ph ⁱ Pr N CH ₃ F IT N N IX-24-6 ^t bu N N CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT N N IX-24-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT N N IX-24-8 ^t bu * n * ⁱ Pr N CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-25-1 Ph H H H ⁱ Pr H CH ₃ F IT n n IX-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ F IT n n IX-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F it n n IX-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F it n n IX-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F it n n IX-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F it n n IX-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F it n n IX-25-8 Ph * H * ⁱ Pr H CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-26-1 p-me-ph H H H ⁱ Pr H CH ₃ F IT N n IX-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ F IT n n IX-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n IX-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n IX-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT n n IX-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n n IX-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n IX-26-8 p-me-ph * H * ⁱ Pr H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-27-1 p-f-ph H H H ⁱ Pr H CH ₃ F IT N n IX-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ F IT N n IX-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n IX-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n IX-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT n n IX-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n n IX-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n IX-27-8 p-f-ph * H * ⁱ Pr H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-28-1 p-Cl-Ph H H H ⁱ Pr H CH ₃ F IT N n IX-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H CH ₃ F IT n n IX-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n IX-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT n n IX-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT n n IX-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT n n IX-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n IX-28-8 p-Cl-Ph * H * ⁱ Pr H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ F IT N n IX-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ F IT N n IX-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n IX-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT N n IX-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT N n IX-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT N n IX-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT n n IX-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-30-1 p-1-ph n n n ⁱ Pr N CH ₃ F IT N N IX-30-2 p-1-ph n N CH ₃ ⁱ Pr N CH ₃ F IT N N IX-30-3 p-1-ph n n CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N IX-30-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT N N IX-30-5 p-1-ph n n CH ₂ Ph TT N CH ₃ F IT N n IX-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT N n IX-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT N n IX-30-8 p-1-ph * n * ⁱ Pr N CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-31-1 CH ₃ N N N ⁿ Bu H CH ₃ F IT N N IX-31-2 CH ₃ N N CH ₃ ⁿ Bu H CH ₃ F IT N N IX-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N n IX-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H CH ₃ F IT N n IX-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N n IX-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N n IX-31-8 CH ₃ * n * ⁿ Bu H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-32-1 Et H H H ⁿ Bu H CH ₃ F IT N N IX-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ F IT N N IX-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N N IX-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N N IX-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N n IX-32-8 Et * H * ⁿ Bu H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-33-1 ⁱ Pr n N N ⁿ Bu H CH ₃ F IT N n GC-33-2 ⁱ Pr N n CH ₃ ⁿ Bu H CH ₃ F IT N n IX-33-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N n IX-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N n IX-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu H CH ₃ F IT N n IX-33-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N n IX-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N n IX-33-8 ⁱ Pr * N * ⁿ Bu H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-34-1 ^t bu N N n ⁿ Bu N CH ₃ F IT n N IX-34-2 ^t bu n N CH ₃ ⁿ Bu n CH ₃ F IT n N IX-34-3 ^t bu n N CH (CH ₃ ) ₂ ⁿ Bu n CH ₃ F IT n n IX-34-4 ^t bu n N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu n CH ₃ F IT n n IX-34-5 ^t bu n n CH ₂ Ph ⁿ Bu n CH ₃ F IT n n IX-34-6 ^t bu n n CH ₂ -indol-3-yl ⁿ Bu n CH ₃ F IT n n IX-34-7 ^t bu n n CH ₂ CH ₂ SCH ₃ ⁿ Bu n CH ₃ F IT n n IX-34-8 ^t bu * n * ⁿ Bu n CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-35-1 Ph H H H ⁿ Bu H CH ₃ F IT N N IX-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N IX-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N N IX-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N N IX-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N N IX-35-8 Ph * H * ⁿ Bu H CH ₃ F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-36-1 p-me-ph H H H ⁿ Bu H CH ₃ F IT N N IX-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N IX-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N n IX-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N n IX-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N n IX-36-8 p-me-ph * H * ⁿ Bu H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-37-1 p-f-ph H H H ⁿ Bu H CH ₃ F IT N N IX-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N IX-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N N IX-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N n IX-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N n IX-37-8 p-f-ph * H * ⁿ Bu H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ F IT N N IX-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N IX-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT n N IX-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT n N IX-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT n n IX-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT n n IX-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT n n IX-38-8 p-Cl-Ph * H * ⁿ Bu H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ F IT N N IX-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT N N IX-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT N N IX-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT N N IX-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT N N IX-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-40-1 p-1-ph N N n ⁿ Bu H CH ₃ F IT N N IX-40-2 p-1-ph N N CH ₃ ⁿ Bu H CH ₃ F IT N N IX-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-40-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT N N IX-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H CH ₃ F IT N N IX-40-6 p-1-ph n n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT n N IX-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT n N IX-40-8 p-1-ph * n * ⁿ Bu H CH ₃ F IT n N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ 1X-4Y CH ₃ N n n Bz H CH ₃ F IT N n IX-41-2 CH ₃ N n CH ₃ Bz H CH ₃ F IT N n IX-41-3 CH ₃ n n CH (CH ₃ ) ₂ Bz H CH ₃ F IT n n IX-41-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n n IX-41-5 CH ₃ n n CH ₂ Ph Bz H CH ₃ F IT n n IX-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz H CH ₃ F IT n n IX-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n IX-41-8 CH ₃ * n * Bz H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-42-1 Et H H H Bz H CH ₃ F IT N N IX-42-2 Et H H CH ₃ Bz H CH ₃ F IT N N IX-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-42-5 Et H H CH ₂ Ph Bz H CH ₃ F IT N n IX-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ F IT N n IX-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n IX-42-8 Et * H * Bz H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-43-1 ⁱ Pr N N N Bz H CH ₃ F IT N N IX-43-2 ⁱ Pr N N CH ₃ Bz H CH ₃ F IT N N IX-43-3 fpr N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT n N IX-43-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n N IX-43-5 ⁱ Pr N N CH ₂ Ph Bz H CH ₃ F IT n n IX-43-6 ⁱ Pr N N CH ₂ -indol-3-yl Bz H CH ₃ F IT n n IX-43-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n IX-43-8 ⁱ Pr * N * Bz H CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-44-1 ^t bu N N n Bz H CH ₃ F IT N N IX-44-2 ^t bu N N CH ₃ Bz H CH ₃ F IT N N IX-44-3 ^t bu N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-44-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-44-5 ^t bu N N CH ₂ Ph Bz H CH ₃ F IT N. n IX-44-6 ^t bu N N CH ₂ -indol-3-yl Bz H CH ₃ F IT N n IX-44-7 ^t bu N N CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n IX-44-8 ^t bu * N * Bz H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-45-1 Ph H H H Bz H CH ₃ F IT N N IX-45-2 Ph H H CH ₃ Bz H CH ₃ F IT N N IX-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N IX-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N IX-45-5 Ph H H CH ₂ Ph Bz H CH ₃ F IT N N IX-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT N N IX-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n IX-45-8 Ph * H * Bz H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-46-1 p-me-ph H H H Bz H CH ₃ F IT N n IX-46-2 p-me-ph H H CH ₃ Bz H CH ₃ F IT N n IX-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT n n IX-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ F IT n n IX-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT n n IX-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n IX-46-8 p-me-ph * H * Bz H CH ₃ F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-47-1 p-f-ph H H H Bz H CH ₃ F IT N n IX-47-2 p-f-ph H H CH ₃ Bz H CH ₃ F IT N n IX-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ F IT n n IX-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT n n IX-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n n IX-47-8 p-f-ph * H * Bz H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-48-1 p-Cl-Ph H H H Bz H CH ₃ F IT N N IX-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ F IT N N IX-48-3 p-CI-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ F IT N n IX-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT N n IX-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n IX-48-8 p-Cl-Ph * H * Bz H CH ₃ F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table IX-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-49-1 p-Br-Ph H H H Bz H CH ₃ F IT N N IX-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ F IT N N IX-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N IX-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N N IX-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ F IT N N IX-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT N N IX-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT n N IX-49-8 p-Br-Ph * H * Bz H CH ₃ F IT n N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table IX-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ IX-50-1 p-1-ph N N n Bz H CH ₃ F IT N n IX-50-2 p-1-ph N N CH ₃ Bz H CH ₃ F IT N n IX-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT N n IX-50-5 p-1-ph N n CH ₂ Ph Bz H CH ₃ F IT N n IX-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H CH ₃ F IT N n IX-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT N n IX-50-8 p-1-ph * n * Bz H CH ₃ F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-1-1 CH ₃ N N N CH ₃ N F F IT n n X-1-2 CH ₃ N N CH ₃ CH ₃ N F F IT n n X-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-1-5 CH ₃ N N CH ₂ Ph CH ₃ N F F IT n n X-1-6 CH ₃ N N CH ₂ -indol-3-yl CH ₃ N F F IT n n X-1-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT n n X-1-8 CH ₃ * N * CH ₃ N F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-2-1 Et H H H CH ₃ N F F IT n n X-2-2 Et H H CH ₃ CH ₃ n F F IT n n X-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-2-5 Et H H CH ₂ Ph CH ₃ n F F IT n n X-2-6 Et H H CH ₂ -indol-3-yl CH ₃ n F F IT n n X-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n X-2-8 Et * H * CH ₃ n F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-3-1 ^t Pr H H H CH ₃ n F F IT N N X-3-2 ^t Pr H H CH ₃ CH ₃ n F F IT N N hz ^t Pr H H CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-3-4 ^t Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-3-5 ^t Pr H H CH ₂ Ph CH ₃ n F F IT n n X-3-6 ^t Pr H H CH ₂ -indol-3-yl CH ₃ n F F IT n n X-3-7 ^t Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n X-3-8 ^t Pr * H * CH ₃ n F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-4-1 ^t Bu H H H CH ₃ n F F IT N n X-4-2 ^t Bu H H CH ₃ CH ₃ n F F IT N n X-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ n F F IT N n X-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-4-5 ^t Bu H H CH ₂ Ph CH ₃ n F F it n n X-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ n F F it n n X-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F it n n X-4-8 ^t Bu * H * CH ₃ n F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-5. No. R R R R ^3b R R R X Y R R X-5-1 Ph N N n CH ₃ N F F IT N n X-5-2 Ph N N CH ₃ CH ₃ N F F IT N n X-5-3 Ph N N CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-5-4 Ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-5-5 Ph N n CH ₂ Ph CH ₃ N F F IT n n X-5-6 Ph N n CH ₂ -indol-3-yl CH ₃ n F F IT n n X-5-7 Ph N n CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n X-5-8 Ph * n * CH ₃ n F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-6-1 p-me-ph H H H CH ₃ N F F IT N N X-6-2 p-me-ph H H CH ₃ CH ₃ N F F IT N N X-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT N N X-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT N N X-6-5 p-me-ph H H CH ₂ Ph CH ₃ N F F IT N N X-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n F F IT N N X-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT N N X-6-8 p-me-ph * H CH ₃ n F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-7-1 p-f-ph H H H CH ₃ N F F IT N n X-7-2 p-f-ph H H CH ₃ CH ₃ n F F IT N n X-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-7-6 p-f-ph H H CH ₂ Ph CH ₃ n F F IT n n X-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n F F IT n n X-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT n n X-7-20 p-f-ph * H * CH ₃ n F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-8-1 p-Cl-Ph H H H CH ₃ N F F IT N N X-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F F IT N N X-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT N n X-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT N n X-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N F F IT N n X-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N F F IT N n X-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT N n X-8-8 p-Cl-Ph * H * CH ₃ N F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-9-1 p-Br-Ph H H H CH ₃ N F F IT N n X-9-2 p-Br-Ph H H CH ₃ CH ₃ N F F IT n n X-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F F it n n X-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N F F it n n X-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F it n n X-9-20 p-Br-Ph * H * CH ₃ N F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-10-1 p-1-ph n N n CH ₃ N F F IT n N X-10-2 p-1-ph N n CH ₃ CH ₃ N F F IT n N X-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ N F F IT n n X-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT n n X-10-5 p-1-ph n n CH ₂ Ph CH ₃ n F F IT n n X-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ n F F it n n X-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ n F F it n n X-10-8 p-1-ph * n * CH ₃ n F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-11-1 CH ₃ N n n Et H F F OH H H X-11-2 CH ₃ N n CH ₃ Et H F F OH H H X-11-3 CH ₃ n n CH (CH ₃ ) ₂ Et H F F OH H H X-11-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-11-5 CH ₃ n n CH ₂ Ph Et H F F OH H H X-11-6 CH ₃ n n CH ₂ -indol-3-yl Et H F F OH H H X-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-11-8 CH ₃ * n * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-12-1 Et H H H Et H F F OH H H X-12-2 Et H H CH ₃ Et H F F OH H H X-12-3 Et H H CH (CH ₃ ) ₂ Et H F F OH H H X-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-12-5 Et H H CH ₂ Ph Et H F F OH H H X-12-6 Et H H CH ₂ -indol-3-yl Et H F F OH H H X-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-12-8 Et * H * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-13-1 ⁱ Pr n n n Et H F F OH H H X-13-2 ⁱ Pr N n CH ₃ Et H F F OH H H X-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H F F OH H H X-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-13-5 ⁱ Pr N n CH ₂ Ph Et H F F OH H H X-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H F F OH H H X-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-13-8 ⁱ Pr * n * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-14-1 ^t bu N n n Et H F F OH H H X-14-2 ^t bu N n CH ₃ Et H F F OH H H X-14-3 ^t bu n n CH (CH ₃ ) ₂ Et H F F OH H H X-14-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-14-5 ^t bu n n CH ₂ Ph Et H F F OH H H X-14-6 ^t bu n n CH ₂ -indol-3-yl Et H F F OH H H X-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-14-8 ^t bu * n * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-15-1 Ph H H H Et H F F OH H H X-15-2 Ph H H CH ₃ Et H F F OH H H X-15-3 Ph H H CH (CH ₃ ) ₂ Et H F F OH H H X-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-15-5 Ph H H CH ₂ Ph Et H F F OH H H X-15-6 Ph H H CH ₂ -indol-3-yl Et H F F OH H H X-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-15-8 Ph * H * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-16-1 p-me-ph H H H Et H F F OH H H X-16-2 p-me-ph H H CH ₃ Et H F F OH H H X-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F F OH H H X-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-16-5 p-me-ph H H CH ₂ Ph Et H F F OH H H X-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F F OH H H X-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-16-8 p-me-ph * H * Et H F F OH H H

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-17-1 p-f-ph H H H Et H F F OH H H X-17-2 p-f-ph H H CH ₃ Et H F F OH H H X-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F F OH H H X-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-17-5 p-f-ph H H CH ₂ Ph Et H F F OH H H X-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F F OH H H X-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-17-8 p-f-ph * H * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-18-1 p-Cl-Ph H H H Et H F F OH H H X-18-2 p-Cl-Ph H H CH ₃ Et H F F OH H H X-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F F OH H H X-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-18-5 p-Cl-Ph H H CH ₂ Ph Et H F F OH H H X-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F F OH H H X-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-18-8 p-Cl-Ph * H * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-19-1 p-Br-Ph H H H Et H F F OH H H X-19-2 p-Br-Ph H H CH ₃ Et H F F OH H H X-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F F OH H H X-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH H H X-19-5 p-Br-Ph H H CH ₂ Ph Et H F F OH H H X-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F F OH H H X-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH H H X-19-8 p-Br-Ph * H * Et H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ X-20-1 p-1-ph N n n Et H F F OH H X-20-2 p-1-ph N n CH ₃ Et H F F OH H X-20-3 p-1-ph n n CH (CH ₃ ) ₂ Et H F F OH H X-20-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ Et H F F OH H X-20-5 p-1-ph n n CH ₂ Ph Et H F F OH H X-20-6 p-1-ph n n CH ₂ -indol-3-yl Et H F F OH H X-20-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Et H F F OH H X-20-8 p-1-ph * n * Et H F F OH H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-21-1 CH ₃ N N n ⁱ Pr N F F IT N N X-21-2 CH ₃ N n CH ₃ ⁱ Pr N F F IT N N X-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr N F F IT N N X-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT N N X-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N F F IT N N X-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N F F IT N N X-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT N N X-21-8 CH ₃ * n * ⁱ Pr N F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-22-1 Et H H H ⁱ Pr H F F OH H H X-22-2 Et H H CH ₃ ⁱ Pr H F F OH H H X-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-22-5 Et H H CH ₂ Ph ⁱ Pr H F F OH H H X-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-22-8 Et * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-23-1 ⁱ Pr N N n ⁱ Pr N F F IT N n X-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N F F IT N n X-23-3 ⁱ Pr n N CH (CH ₃ ) ₂ ⁱ Pr n F F IT N n X-23-4 ⁱ Pr n N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F F IT N n X-23-5 ⁱ Pr n N CH ₂ Ph ⁱ Pr n F F IT n n X-23-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr n F F IT n n X-23-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F F IT n n X-23-8 ⁱ Pr * n * ⁱ Pr n F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-24-1 ⁿ Bu N n n ⁱ Pr N F F IT N N X-24-2 ⁿ Bu N n CH ₃ ⁱ Pr N F F IT N N X-24-3 ⁿ Bu N n CH (CH ₃ ) ₂ ⁱ Pr N F F IT N N X-24-4 ⁿ Bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT N N X-24-5 ⁿ Bu N n CH ₂ Ph ⁱ Pr N F F IT N N X-24-6 ⁿ Bu n n CH ₂ -indol-3-yl ⁱ Pr N F F IT N N X-24-7 ⁿ Bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT N N X-24-8 ⁿ Bu n * ⁱ Pr N F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-25-1 Ph H H H ⁱ Pr H F F OH H H X-25-2 Ph H H CH ₃ ⁱ Pr H F F OH H H X-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-25-5 Ph H H CH ₂ Ph ⁱ Pr H F F OH H H X-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-25-8 Ph * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-26-1 p-me-ph H H H ⁱ Pr H F F OH H H X-26-2 p-me-ph H H CH ₃ ⁱ Pr H F F OH H H X-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F F OH H H X-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-26-8 p-me-ph * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-27-1 p-f-ph H H H ⁱ Pr H F F OH H H X-27-2 p-f-ph H H CH ₃ ⁱ Pr H F F OH H H X-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F F OH H H X-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-27-8 p-f-ph * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-28-1 p-Cl-Ph H H H ⁱ Pr H F F OH H H X-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F F OH H H X-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F F OH H H X-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-28-8 p-Cl-Ph * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-29-1 p-Br-Ph H H H ⁱ Pr H F F OH H H X-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F F OH H H X-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F F OH H H X-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-29-8 p-Br-Ph * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-30-1 p-i-ph H H H ⁱ Pr H F F OH H H X-30-2 p-i-ph H H CH ₃ ⁱ Pr H F F OH H H X-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH H H X-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H F F OH H H X-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH H H X-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH H H X-30-8 p-i-ph * H * ⁱ Pr H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-31-1 CH ₃ N N N ⁿ Bu H F F OH H H X-31-2 CH ₃ N N CH ₃ ⁿ Bu H F F OH H H X-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H F F OH H H X-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-31-8 CH ₃ * N * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-32-1 Et H H H ⁿ Bu H F F OH H H X-32-2 Et H H CH ₃ ⁿ Bu H F F OH H H X-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-32-5 Et H H CH ₂ Ph ⁿ Bu H F F OH H H X-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-32-8 Et * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-33-1 ⁱ Pr H H H ⁿ Bu H F F OH H H X-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H F F OH H H X-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H F F OH H H X-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-33-8 ⁱ Pr * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-34-1 ⁿ Bu H H H ⁿ Bu H F F OH H H X-34-2 ⁿ Bu H H CH ₃ ⁿ Bu H F F OH H H X-34-3 ⁿ Bu H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-34-4 ⁿ Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-34-5 ⁿ Bu H H CH ₂ Ph ⁿ Bu H F F OH H H X-34-6 ⁿ Bu H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-34-7 ⁿ Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-34-8 ⁿ Bu * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-35-1 Ph H H H ⁿ Bu H F F OH H H X-35-2 Ph H H CH ₃ ⁿ Bu H F F OH H H X-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-35-5 Ph H H CH ₂ Ph ⁿ Bu H F F OH H H X-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-35-8 Ph * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-36-1 p-me-ph H H H ⁿ Bu H F F OH H H X-36-2 p-me-ph H H CH ₃ ⁿ Bu H F F OH H H X-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F F OH H H X-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H n X-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-36-8 p-me-ph * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-37-1 p-f-ph H H H ⁿ Bu H F F OH H H X-37-2 p-f-ph H H CH ₃ ⁿ Bu H F F OH H H X-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F F OH H H X-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-37-8 p-f-ph * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-38-1 p-Cl-Ph H H H ⁿ Bu H F F OH H H X-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F F OH H H X-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F F OH H H X-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-38-8 p-Cl-Ph * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-39-1 p-Br-Ph H H H ⁿ Bu H F F OH H H X-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F F OH H H X-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F F OH H H X-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-39-8 p-Br-Ph * H * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-40-1 p-1-ph N n n ⁿ Bu H F F OH H H X-40-2 p-1-ph N n CH ₃ ⁿ Bu H F F OH H H X-40-3 p-1-ph n n CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-40-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH H H X-40-5 p-1-ph n n CH ₂ Ph ⁿ Bu H F F OH H H X-40-6 p-1-ph n n CH ₂ -indol-3-yl ⁿ Bu H F F OH H H X-40-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH H H X-40-8 p-1-ph * n * ⁿ Bu H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-4-1 CH ₃ N n n Bz H F F OH H H X-41-2 CH ₃ N n CH ₃ Bz H F F OH H H X-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H F F OH H H X-41-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-41-5 CH ₃ n n CH ₂ Ph Bz H F F OH H H X-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz H F F OH H H X-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-41-8 CH ₃ * n * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-42-1 Et H H H Bz H F F OH H H X-42-2 Et H H CH ₃ Bz H F F OH H H X-42-3 Et H H CH (CH ₃ ) ₂ Bz H F F OH H H X-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-42-5 Et H H CH ₂ Ph Bz H F F OH H H X-42-6 Et H H CH ₂ -indol-3-yl Bz H F F OH H H X-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-42-8 Et * H * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-43-1 ⁱ Pr N N n Bz H F F OH H H X-43-2 ⁱ Pr N N CH ₃ Bz H F F OH H H X-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H F F OH H H X-43-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-43-5 ⁱ Pr N n CH ₂ Ph Bz H F F OH H H X-43-6 ⁱ Pr N N CH ₂ -indol-3-yl Bz H F F OH H H X-43-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-43-8 ⁱ Pr * N * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-44-1 ^t bu N N n Bz H F F OH H H X-44-2 ^t bu N N CH ₃ Bz H F F OH H H X-44-3 ^t bu N N CH (CH ₃ ) ₂ Bz H F F OH H H X-44-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-44-5 ^t bu N n CH ₂ Ph Bz H F F OH H H X-44-6 ^t bu N n CH ₂ -indol-3-yl Bz H F F OH H H X-44-7 ^t bu N n CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-44-8 ^t bu * n * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-45-1 Ph H H H Bz H F F IT N N X-45-2 Ph H H CH ₃ Bz H F F IT N N X-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F F IT n N X-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F IT n N X-45-5 Ph H H CH ₂ Ph Bz H F F IT n n X-45-6 Ph H H CH ₂ -indol-3-yl Bz H F F IT n n X-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F IT n n X-45-8 Ph * H * Bz H F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-46-1 p-me-ph H H H Bz H F F OH H H X-46-2 p-me-ph H H CH ₃ Bz H F F OH H H X-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F F OH H H X-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-46-5 p-me-ph H H CH ₂ Ph Bz H F F OH H H X-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F F OH H H X-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-46-8 p-me-ph * H * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-47-1 p-f-ph H H H Bz H F F OH H H X-47-2 p-f-ph H H CH ₃ Bz H F F OH H H X-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F F OH H H X-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-47-5 p-f-ph H H CH ₂ Ph Bz H F F OH H H X-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F F OH H H X-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-47-8 p-f-ph * H * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-48-1 p-CI-Ph H H H Bz H F F OH H H X-48-2 p-Cl-Ph H H CH ₃ Bz H F F OH H H X-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F F OH H H X-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F F OH H H X-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F F OH H H X-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-48-8 p-Cl-Ph * H * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table X-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-49-1 p-Br-Ph H H H Bz H F F OH H H X-49-2 p-Br-Ph H H CH ₃ Bz H F F OH H H X-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F F OH H H X-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-49-5 p-Br-Ph H H CH ₂ Ph Bz H F F OH H H X-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F F OH H H X-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-49-8 p-Br-Ph * H * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table X-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ X-50-1 p-i-ph N N n Bz H F F OH H H X-50-2 p-i-ph N N CH ₃ Bz H F F OH H H X-50-3 p-i-ph N N CH (CH ₃ ) ₂ Bz H F F OH H H X-50-4 p-i-ph N N CH ₂ CH (CH ₃ ) ₂ Bz H F F OH H H X-50-5 p-i-ph N N CH ₂ Ph Bz H F F OH H H X-50-6 p-i-ph N N CH ₂ -indol-3-yl Bz H F F OH H H X-50-7 p-i-ph N N CH ₂ CH ₂ SCH ₃ Bz H F F OH H H X-50-8 p-i-ph * n * Bz H F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-1-1 CH ₃ N n n CH ₃ N n F IT N n XI-1-2 CH ₃ N n CH ₃ CH ₃ N n F IT N n XI-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N n F IT N n XI-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT n n XI-1-5 CH ₃ N n CH ₂ Ph CH ₃ N n F IT n n XI-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N n F IT n n XI-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT n n XI-1-8 CH ₃ * n * CH ₃ n n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-2-1 Et H H H CH ₃ N n F IT n n XI-2-2 Et H H CH ₃ CH ₃ N n F IT n n XI-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N n F IT n n XI-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT n n XI-2-5 Et H H CH ₂ Ph CH ₃ N n F IT n n XI-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N n F IT n n XI-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT n n XI-2-8 Et * H * CH ₃ N n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-3-1 ⁱ Pr H H H CH ₃ N n F IT n n XI-3-2 ⁱ Pr H H CH ₃ CH ₃ n n F IT n n XI-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ n n F IT n n XI-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT n n XI-3-S ⁱ Pr H H CH ₂ Ph CH ₃ n n F it n n XI-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ n n F it n n XI-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F it n n XI-3-8 ⁱ Pr * H * CH ₃ n n F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-4-1 ^t bu n N n CH ₃ N N F IT N n XI-4-2 ^t bu n N CH ₃ CH ₃ N N F IT N N XI-4-3 ^t bu N N CH (CH ₃ ) ₂ CH ₃ N N F IT n N XI-4-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT n N XI-4-5 ^t bu N N CH ₂ Ph CH ₃ N N F IT n n XI-4-6 ^t bu N N CH ₂ -indol-3-yl CH ₃ N N F IT n n XI-4-7 ^t bu N N CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n XI-4-8 ^t bu * N * CH ₃ N N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-5-1 Ph H H H CH ₃ N N F IT N N XI-5-2 Ph H H CH ₃ CH ₃ N N F IT N N XI-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT N n XI-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT N n XI-5-5 Ph H H CH ₂ Ph CH ₃ N n F IT N n XI-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N n F IT N n XI-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT N n XI-5-8 Ph * H * CH ₃ N n F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-6-1 p-me-ph H H H CH ₃ N N F IT n n XI-6-2 p-me-ph H H CH ₃ CH ₃ N N F IT n n XI-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT n n XI-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F it n n XI-6-5 p-me-ph H H CH ₂ Ph CH ₃ N N F it n n XI-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N N F it n n XI-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F it n n XI-6-8 p-me-ph * H * CH ₃ N n F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-7-1 p-f-ph H H H CH ₃ N N F it n n XI-7-2 p-f-ph H H CH ₃ CH ₃ N N F it n n XI-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N N F it n n XI-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F it n n XI-7-6 p-f-ph H H CH ₂ Ph CH ₃ N N F it n n XI-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N N F it n n XI-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F it n n XI-7-20 p-f-ph * H * CH ₃ N N F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-8-1 p-Cl-Ph H H H CH ₃ N N F IT N n XI-8-2 p-Cl-Ph H H CH ₃ CH ₃ N N F IT N n XI-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT N n XI-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT n n XI-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N N F IT n n XI-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N N F IT n n XI-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n XI-8-8 p-Cl-Ph * H * CH ₃ n N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-9-1 p-Br-Ph H H H CH ₃ N N F IT n n XI-9-2 p-Br-Ph H H CH ₃ CH ₃ N N F IT n n XI-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT n n XI-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT n n XI-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N N F IT n n XI-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N N F IT n n XI-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n XI-9-20 p-Br-Ph * H * CH ₃ N N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-10-1 p-1-ph N n n CH ₃ N N F IT N n XI-10-2 p-1-ph N n CH ₃ CH ₃ N N F IT N n XI-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ N N F IT N n XI-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT n n XI-10-5 p-1-ph n n CH ₂ Ph CH ₃ N N F IT n n XI-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N N F IT n n XI-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT n n XI-10-8 p-1-ph * n * CH ₃ N N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-11-1 CH ₃ N n n Et H H F OH H H XI-11-2 CH ₃ N n CH ₃ Et H H F OH H H XI-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H H F OH H H XI-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-11-5 CH ₃ n n CH ₂ Ph Et H H F OH H H XI-11-6 CH ₃ n n CH ₂ -indol-3-yl Et H H F OH H H XI-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-11-8 CH ₃ * n * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-12-1 Et H H H Et H H F OH H H XI-12-2 Et H H CH ₃ Et H H F OH H H XI-12-3 Et H H CH (CH ₃ ) ₂ Et H H F OH H H XI-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-12-5 Et H H CH ₂ Ph Et H H F OH H H XI-12-6 Et H H CH ₂ -indol-3-yl Et H H F OH H H XI-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-12-8 Et * H * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-13-1 ⁱ Pr N n n Et H H F OH H H XI-13-2 fpr N n CH ₃ Et H H F OH H H XI-13-3 ⁱ Pr N n CH (CH ₃ ) ₂ Et H H F OH H H XI-13-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-13-5 ⁱ Pr n n CH ₂ Ph Et H H F OH H H XI-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et H H F OH H H XI-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-13-8 ⁱ Pr * n * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-14-1 ^t bu N n n Et H H F OH H H XI-14-2 ^t bu N n CH ₃ Et H H F OH H H XI-14-3 ^t bu N n CH (CH ₃ ) ₂ Et H H F OH H H XI-14-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-14-5 ^t bu n n CH ₂ Ph Et H H F OH H H XI-14-6 ^t bu n n CH ₂ -indol-3-yl Et H H F OH H H XI-14-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-14-8 ^t bu * n * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-15-1 Ph H H H Et H H F OH H H XI-15-2 Ph H H CH ₃ Et H H F OH H H XI-15-3 Ph H H CH (CH ₃ ) ₂ Et H H F OH H H XI-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-15-5 Ph H H CH ₂ Ph Et H H F OH H H XI-15-6 Ph H H CH ₂ -indol-3-yl Et H H F OH H H XI-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-15-8 Ph * H * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-16-1 p-me-ph H H H Et H H F OH H H XI-16-2 p-me-ph H H CH ₃ Et H H F OH H H XI-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H H F OH H H XI-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-16-5 p-me-ph H H CH ₂ Ph Et H H F OH H H XI-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H H F OH H H XI-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-16-8 p-me-ph * H * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-17-1 p-f-ph H H H Et H H F OH H H XI-17-2 p-f-ph H H CH ₃ Et H H F OH H H XI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H H F OH H H XI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-17-5 p-f-ph H H CH ₂ Ph Et H H F OH H H XI-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H H F OH H H XI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-17-8 p-f-ph * H * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-18-1 p-Cl-Ph H H H Et H H F OH H H XI-18-2 p-CI-Ph H H CH ₃ Et H H F OH H H XI-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H H F OH H H XI-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-18-5 p-Cl-Ph H H CH ₂ Ph Et H H F OH H H XI-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H H F OH H H XI-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-18-8 p-Cl-Ph * H * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-19-1 p-Br-Ph H H H Et H H F OH H H XI-19-2 p-Br-Ph H H CH ₃ Et H H F OH H H XI-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H H F OH H H XI-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-19-5 p-Br-Ph H H CH ₂ Ph Et H H F OH H H XI-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H H F OH H H XI-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-19-8 p-Br-Ph * H * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-20-1 p-1-ph N N n Et H H F OH H H XI-20-2 p-1-ph N N CH ₃ Et H H F OH H H XI-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et H H F OH H H XI-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et H H F OH H H XI-20-5 p-1-ph N n CH ₂ Ph Et H H F OH H H XI-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H H F OH H H XI-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H H F OH H H XI-20-8 p-1-ph * n * Et H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-21-1 CH ₃ N N N ⁱ Pr H N F it N n XI-21-2 CH ₃ N N CH ₃ ⁱ Pr n n F IT N n XI-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr n n F IT N n XI-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n n F IT n n XI-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr n n F IT n n XI-21-6 CH ₃ N N CH ₂ -indol-3-yl ⁱ Pr n n F IT n n XI-21-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁱ Pr n n F IT n n XI-21-8 CH ₃ * N * ⁱ Pr n n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-22-1 Et H H H ⁱ Pr H H F OH H H XI-22-2 Et H H CH ₃ ⁱ Pr H H F OH H H XI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-22-5 Et H H CH ₂ Ph ⁱ Pr H H F OH H H XI-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H XI-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H XI-22-8 Et * H * ⁱ Pr H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-23-1 ⁱ Pr N N N ⁱ Pr N N F IT N N XI-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N N F IT N N XI-23-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁱ Pr N N F IT N N XI-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N N F IT N N XI-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr N N F IT N N XI-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr N N F IT N N XI-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N N F IT N N XI-23-8 ⁱ Pr * n * ⁱ Pr N n F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-24-1 ^t bu N N n ⁱ Pr N N F IT N n XI-24-2 ^t bu N N CH ₃ ⁱ Pr N N F IT N n XI-24-3 ^t bu N N CH (CH ₃ ) ₂ ⁱ Pr N n F IT N n XI-24-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N n F IT n n XI-24-5 ^t bu N N CH ₂ Ph ⁱ Pr N n F IT n n XI-24-6 ^t bu N N CH ₂ -indol-3-yl ⁱ Pr N n F IT n n XI-24-7 ^t bu N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N n F IT n n XI-24-8 ^t bu * n * ⁱ Pr N n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-25-1 Ph H H H ⁱ Pr H H F OH H H XI-25-2 Ph H H CH ₃ ⁱ Pr H H F OH H H XI-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-25-5 Ph H H CH ₂ Ph ⁱ Pr H H F OH H H XI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H XI-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H XI-25-8 Ph * H * ⁱ Pr H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-26-1 p-me-ph H H H ⁱ Pr H H F OH H H XI-26-2 p-me-ph H H CH ₃ ⁱ Pr H H F OH H H XI-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H H F OH H H XI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H XI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H XI-26-8 p-me-ph * H * ⁱ Pr H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-27-1 p-f-ph H H H ⁱ Pr H H F OH H H XI-27-2 p-f-ph H H CH ₃ ⁱ Pr H H F OH H H XI-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H H F OH H H XI-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H XI-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H XI-27-8 p-f-ph * H * ⁱ Pr H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-28-1 p-Cl-Ph H H H ^t Pr H H F OH H H XI-28-2 p-Cl-Ph H H CH ₃ Vr H H F OH H H XI-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ^t Pr H H F OH H H XI-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ^t Pr H H F OH H H XI-28-5 p-Cl-Ph H H CH ₂ Ph * Pr H H F OH H H XI-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ^t Pr H H F OH H H XI-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ^t Pr H H F OH H H XI-28-8 p-Cl-Ph * H * ^t Pr H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-29-1 p-Br-Ph H H H ⁱ Pr H H F OH H H XI-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H H F OH H H XI-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH H H XI-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H H F OH H H XI-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH H H XI-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH H H XI-29-8 p-Br-Ph * H * ⁱ Pr H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-30-1 p-1-ph N n n ⁱ Pr N N F IT N N XI-30-2 p-1-ph N n CH ₃ ⁱ Pr N N F IT N N XI-30-3 p-1-ph n n CH (CH ₃ ) ₂ ⁱ Pr n N F IT N N XI-30-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n N F IT N N XI-30-5 p-1-ph n n CH ₂ Ph ⁱ Pr n N F IT N N XI-30-6 p-1-ph n n CH ₂ -indol-3-yl ⁱ Pr n N F IT n n XI-30-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n n F IT n n XI-30-8 p-1-ph * n * ⁱ Pr n n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-31-1 CH ₃ N N n ⁿ Bu H H F OH H H XI-31-2 CH ₃ N N CH ₃ ⁿ Bu H H F OH H H XI-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H H F OH H H XI-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-31-8 CH ₃ * N * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-32-1 Et H H H ⁿ Bu H H F OH H H XI-32-2 Et H H CH ₃ ⁿ Bu H H F OH H H XI-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-32-5 Et H H CH ₂ Ph ⁿ Bu H H F OH H H XI-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-32-8 Et * H * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-33-1 ⁱ Pr n N N ⁿ Bu H H F OH H H XI-33-2 ⁱ Pr N N CH ₃ ⁿ Bu H H F OH H H XI-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu H H F OH H H XI-33-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-33-8 ⁱ Pr * n * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-34-1 ^t bu N N n ⁿ Bu N N F IT N n XI-34-2 ^t bu N n CH ₃ ⁿ Bu N N F IT N n XI-34-3 ^t bu N n CH (CH ₃ ) ₂ ⁿ Bu N N F IT N n XI-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N N F IT N n XI-34-5 ^t bu N n CH ₂ Ph ⁿ Bu N N F IT N n XI-34-6 ^t bu n n CH ₂ -indol-3-yl ⁿ Bu N N F IT N n XI-34-7 ^t bu n N CH ₂ CH ₂ SCH ₃ ⁿ Bu N N F IT N n XI-34-8 ^t bu * N * ⁿ Bu N N F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-35-1 Ph H H H ⁿ Bu H H F OH H H XI-35-2 Ph H H CH ₃ ⁿ Bu H H F OH H H XI-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-35-5 Ph H H CH ₂ Ph ⁿ Bu H H F OH H H XI-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-35-8 Ph * H * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-36-1 p-me-ph H H H ⁿ Bu H H F OH H H XI-36-2 p-me-ph H H CH ₃ ⁿ Bu H H F OH H H XI-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H H F OH H H XI-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-36-8 p-me-ph * H * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-37-1 p-f-ph H H H ⁿ Bu H H F OH H H XI-37-2 p-f-ph H H CH ₃ ⁿ Bu H H F OH H H XI-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H H F OH H H XI-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-37-8 p-f-ph * H * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-38-1 p-Cl-Ph H H H ⁿ Bu H H F OH H H XI-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H H F OH H H XI-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H H F OH H H XI-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-38-8 p-Cl-Ph * H * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-39-1 p-Br-Ph H H H ⁿ Bu H H F OH H H XI-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H H F OH H H XI-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H H F OH H H XI-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-39-8 p-Br-Ph * H * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-40-1 p-1-ph N N n ⁿ Bu H H F OH H H XI-40-2 p-1-ph N N CH ₃ ⁿ Bu H H F OH H H XI-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH H H XI-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H H F OH H H XI-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H H F OH H H XI-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH H H XI-40-8 p-1-ph * n * ⁿ Bu H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-41-1 CH ₃ N N n Bz H H F OH H H XI-41-2 CH ₃ N N CH ₃ Bz H H F OH H H XI-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H H F OH H H XI-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-41-5 CH ₃ N n CH ₂ Ph Bz H H F OH H H XI-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H H F OH H H XI-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-41-8 CH ₃ * n * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-42-1 Et H H H Bz H H F OH H H XI-42-2 Et H H CH ₃ Bz H H F OH H H XI-42-3 Et H H CH (CH ₃ ) ₂ Bz H H F OH H H XI-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-42-5 Et H H CH ₂ Ph Bz H H F OH H H XI-42-6 Et H H CH ₂ -indol-3-yl Bz H H F OH H H XI-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-42-8 Et * H * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-43-1 ⁱ Pr N n n Bz H H F OH H H XI-43-2 ⁱ Pr N n CH ₃ Bz H H F OH H H XI-43-3 ⁱ Pr n n CH (CH ₃ ) ₂ Bz H H F OH H H XI-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-43-5 ⁱ Pr n n CH ₂ Ph Bz H H F OH H H XI-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz H H F OH H H XI-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-43-8 ⁱ Pr * n * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-44-1 ^t bu N n n Bz H H F OH H H XI-44-2 ^t bu N n CH ₃ Bz H H F OH H H XI-44-3 ^t bu n n CH (CH ₃ ) ₂ Bz H H F OH H H XI-44-4 ^t bu n n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-44-5 ^t bu n n CH ₂ Ph Bz H H F OH H H XI-44-6 ^t bu n n CH ₂ -indol-3-yl Bz H H F OH H H XI-44-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-44-8 ^t bu * n * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-45-1 Ph H H H Bz H H F OH H H XI-45-2 Ph H H CH ₃ Bz H H F OH H H XI-45-3 Ph H H CH (CH ₃ ) ₂ Bz H H F OH H H XI-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-45-5 Ph H H CH ₂ Ph Bz H H F OH H H XI-45-6 Ph H H CH ₂ -indol-3-yl Bz H H F OH H H XI-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-45-8 Ph * H * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-46-1 p-me-ph H H H Bz H H F OH H H XI-46-2 p-me-ph H H CH ₃ Bz H H F OH H H XI-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H H F OH H H XI-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-46-5 p-me-ph H H CH ₂ Ph Bz H H F OH H H XI-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H H F OH H H XI-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-46-8 p-me-ph * H * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-47-1 p-f-ph H H H Bz H H F OH H H XI-47-2 p-f-ph H H CH ₃ Bz H H F OH H H XI-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H H F OH H H XI-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-47-5 p-f-ph H H CH ₂ Ph Bz H H F OH H H XI-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H H F OH H H XI-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-47-8 p-f-ph * H Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-48-1 p-Cl-Ph H H H Bz H H F OH H H XI-48-2 p-Cl-Ph H H CH ₃ Bz H H F OH H H XI-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H H F OH H H XI-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-48-5 p-Cl-Ph H H CH ₂ Ph Bz H H F OH H H XI-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H H F OH H H XI-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-48-8 p-Cl-Ph * H * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XI-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-49-1 p-Br-Ph H H H Bz H H F OH H H XI-49-2 p-Br-Ph H H CH ₃ Bz H H F OH H H XI-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H H F OH H H XI-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-49-5 p-Br-Ph H H CH ₂ Ph Bz H H F OH H H XI-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H H F OH H H XI-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-49-8 p-Br-Ph * H * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XI-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XI-50-1 p-1-ph N n n Bz H H F OH H H XI-50-2 p-1-ph N n CH ₃ Bz H H F OH H H XI-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz H H F OH H H XI-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH H H XI-50-5 p-1-ph N n CH ₂ Ph Bz H H F OH H H XI-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H H F OH H H XI-50-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Bz H H F OH H H XI-50-8 p-1-ph * n * Bz H H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-1-1 CH ₃ N N N CH ₃ N ₃ F F IT N N XII-1-2 CH ₃ N N CH ₃ CH ₃ N ₃ F F IT N N XII-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT N N XII-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT N N XII-1-5 CH ₃ N n CH ₂ Ph CH ₃ N ₃ F F IT N N XII-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N ₃ F F IT n N XII-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F IT n n XII-1-8 CH ₃ * n * CH ₃ N ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-2-1 Et H H H CH ₃ N ₃ F F IT n N XII-2-2 Et H H CH ₃ CH ₃ N ₃ F F IT n n XII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT n n XII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT n n XII-2-5 Et H H CH ₂ Ph CH ₃ N ₃ F F IT n n XII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N ₃ F F IT n n XII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F IT n n XII-2-8 Et * H * CH ₃ N ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-3-1 ⁱ Pr H H H CH ₃ N ₃ F F IT n n XII-3-2 ⁱ Pr H H CH ₃ CH ₃ N ₃ F F IT n n XII-3-Z ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT n n XII-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT n n XII-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ N ₃ F F IT n n XII-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ N ₃ F F it n n XII-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F it n n XII-3-8 ⁱ Pr * H * CH ₃ N ₃ F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-4-1 ^t Bu H H H CH ₃ N ₃ F F IT n N XII-4-2 ^t Bu H H CH ₃ CH ₃ N ₃ F F IT n N XII-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F it n n XII-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F it n n XII-4-5 ^t Bu H H CH ₂ Ph CH ₃ N ₃ F F it n n XII-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ N ₃ F F it n n XII-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F it n n XII-4-8 ^t Bu * H * CH ₃ N ₃ F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-5-1 Ph H H H CH ₃ N ₃ F F IT n n XII-5-2 Ph H H CH ₃ CH ₃ N ₃ F F IT n n XII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT n n XII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT n n XII-5-5 Ph H H CH ₂ Ph CH ₃ N ₃ F F IT n n XII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F F IT n n XII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F IT n n XII-5-8 Ph * H * CH ₃ N ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-6-1 p-me-ph H H H CH ₃ N ₃ F F IT N n XII-6-2 p-me-ph H H CH ₃ CH ₃ N ₃ F F IT N n XII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT N n XII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT N n XII-6-5 p-me-ph H H CH ₂ Ph CH ₃ N ₃ F F IT N n XII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F F IT N n XII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F IT N n XII-6-8 p-me-ph * H * CH ₃ N ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-7-1 p-f-ph H H H CH ₃ N ₃ F F IT N n XII-7-2 p-f-ph H H CH ₃ CH ₃ N ₃ F F IT N n XII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT N n XII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F IT N n XII-7-6 p-f-ph H H CH ₂ Ph CH ₃ N ₃ F F IT N n XII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F F IT N n XII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F IT N n XII-7-20 p-f-ph * H * CH ₃ N ₃ F F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-8-1 p-Cl-Ph H H H CH ₃ N ₃ F F OH H H XII-8-2 p-Cl-Ph H H CH ₃ CH ₃ N ₃ F F OH H H XII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F OH H H XII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F OH H H XII-8-5 p-Cl-Ph H H SNgRp CH ₃ N ₃ F F OH H H XII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F F OH H H XII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F OH H H XII-8-8 p-Cl-Ph * H * CH ₃ N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-9-1 p-Br-Ph H H N CH ₃ N ₃ F F OH H H XII-9-2 p-Br-Ph H H CH ₃ CH ₃ N ₃ F F OH H H XII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F OH H H XII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F OH H H XII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N ₃ F F OH H H XII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F F OH H H XII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F OH H H XII-9-20 p-Br-Ph * H * CH ₃ N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-10-1 p-i-ph H H N CH ₃ N ₃ F F OH H H XII-10-2 p-i-ph H H CH ₃ CH ₃ N ₃ F F OH H H XII-10-3 p-i-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F F OH H H XII-10-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F F OH H H XII-10-5 p-i-ph H H CH ₂ Ph CH ₃ N ₃ F F OH H H XII-10-6 p-i-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F F OH H H XII-10-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F F OH H H XII-10-8 p-i-ph * H * CH ₃ N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-11-1 CH ₃ H H H Et N ₃ F F OH H H XII-11-2 CH ₃ H H CH ₃ Et N ₃ F F OH H H XII-11-3 CH ₃ H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-11-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-11-5 CH ₃ H H CH ₂ Ph Et N ₃ F F OH H H XII-11-6 CH ₃ H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-11-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-11-8 CH ₃ * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-12-1 Et H H H Et N ₃ F F OH H H XII-12-2 Et H H CH ₃ Et N ₃ F F OH H H XII-12-3 Et H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-12-5 Et H H CH ₂ Ph Et N ₃ F F OH H H XII-12-6 Et H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-12-8 Et * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-13-1 ⁱ Pr H H H Et N ₃ F F OH H H XII-13-2 ⁱ Pr H H CH ₃ Et N ₃ F F OH H H XII-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-13-5 ⁱ Pr H H CH ₂ Ph Et N ₃ F F OH H H XII-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-13-8 ⁱ Pr * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-14-1 ^t bu H H H Et N ₃ F F OH H H XII-14-2 ^t bu H H CH ₃ Et N ₃ F F OH H H Xii-3 ^t bu H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-14-4 ^t bu H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-14-5 ^t bu H H CH ₂ Ph Et N ₃ F F OH H H XII-14-6 ^t bu H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-14-7 ^t bu H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-14-8 ^t bu * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-15-1 Ph H H H Et N ₃ F F OH H H XII-15-2 Ph H H CH ₃ Et N ₃ F F OH H H XII-15-3 Ph H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-15-5 Ph H H CH ₂ Ph Et N ₃ F F OH H H XII-15-6 Ph H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-15-8 Ph * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-16-1 p-me-ph H H H Et N ₃ F F OH H H XII-16-2 p-me-ph H H CH ₃ Et N ₃ F F OH H H XII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-16-5 p-me-ph H H CH ₂ Ph Et N ₃ F F OH H H XII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-16-8 p-me-ph * H * Et N ₃ F F OH H H

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-17-1 p-f-ph H H H Et N ₃ F F OH H H XII-17-2 p-f-ph H H CH ₃ Et N ₃ F F OH H H XII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-17-5 p-f-ph H H CH ₂ Ph Et N ₃ F F OH H H XII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-17-8 p-f-ph * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-18-1 p-Cl-Ph H H H Et N ₃ F F OH H H XII-18-2 p-Cl-Ph H H CH ₃ Et N ₃ F F OH H H XII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-18-5 p-Cl-Ph H H CH ₂ Ph Et N ₃ F F OH H H XII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-18-8 p-Cl-Ph * H Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-19-1 p-Br-Ph H H H Et N ₃ F F OH H H XII-19-2 p-Br-Ph H H CH ₃ Et N ₃ F F OH H H XII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H H XII-19-5 p-Br-Ph H H CH ₂ Ph Et N ₃ F F OH H H XII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et N ₃ F F OH H H XII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H H XII-19-8 p-Br-Ph * H * Et N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ XII-20-1 p-1-ph N N n Et N ₃ F F OH H XII-20-2 p-1-ph N N CH ₃ Et N ₃ F F OH H XII-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et N ₃ F F OH H XII-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ F F OH H XII-20-5 p-1-ph N n CH ₂ Ph Et N ₃ F F OH H XII-20-6 p-1-ph N n CH ₂ -indol-3-yl Et N ₃ F F OH H XII-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et N ₃ F F OH H XII-20-8 p-1-ph * n * Et N ₃ F F OH H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-21-1 CH ₃ N N n ⁱ Pr N ₃ F F IT N n XII-21-2 CH ₃ N N CH ₃ ⁱ Pr N ₃ F F IT N n XII-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F IT N n XII-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F IT N n XII-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N ₃ F F IT N n XII-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N ₃ F F IT N n XII-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F IT n n XII-21-8 CH ₃ * n * ⁱ Pr N ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-22-1 Et H H H ⁱ Pr N ₃ F F OH H H XII-22-2 Et H H CH ₃ ⁱ Pr N ₃ F F OH H H XII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-22-5 Et H H CH ₂ Ph ⁱ Pr N ₃ F F OH H H XII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F F OH H H XII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F OH H H XII-22-8 Et * H * ⁱ Pr N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-23. No. R R R * R R R X Y R R XII-23-1 ⁱ Pr N N N ⁱ Pr N ₃ F F IT n n XII-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N ₃ F F IT n n XII-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F it n n XII-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F it n n XII-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr N ₃ F F it n n XII-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁱ Pr N ₃ F F it n n XII-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F it n n XII-23-8 ⁱ Pr * N * ⁱ Pr N ₃ F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-24-1 ^t bu H H H ⁱ Pr N ₃ F F OH H H XII-24-2 ^t bu H H CH ₃ ⁱ Pr N ₃ F F OH H H XII-24-3 ^t bu H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-24-4 ^t bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-24-5 ^t bu H H CH ₂ Ph ⁱ Pr N ₃ F F OH H H XII-24-6 ^t bu H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F F OH H H XII-24-7 ^t bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F OH H H XII-24-8 ^t bu * H * ⁱ Pr N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-25-1 Ph H H H ⁱ Pr N ₃ F F OH H H XII-25-2 Ph H H CH ₃ ⁱ Pr N ₃ F F OH H H XII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-25-5 Ph H H CH ₂ Ph ⁱ Pr N ₃ F F OH H H XII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F F OH H H XII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F OH H H XII-25-8 Ph * H * ⁱ Pr N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ XII-26-1 p-me-ph H H H ⁱ Pr N ₃ F F OH H H XII-26-2 p-me-ph H H CH ₃ ⁱ Pr N ₃ F F OH H H XII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr N ₃ F F OH H H XII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F F OH H H XII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F OH H H XII-26-8 p-me-ph * H * ⁱ Pr N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-27-1 p-f-ph H H H ⁱ Pr N ₃ F F OH H H XII-27-2 p-f-ph H H CH ₃ ⁱ Pr N ₃ F F OH H H XII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H HI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr N ₃ F F OH H H XII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F F OH H H XII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F OH H H XII-27-8 p-f-ph * H * ⁱ Pr N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-28-1 p-Cl-Ph H H H ⁱ Pr N ₃ F F OH H H XII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr N ₃ F F OH H H XII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F OH H H XII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr N ₃ F F OH H H XII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F F OH H H XII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F OH H H XII-28-8 p-Cl-Ph * H * ⁱ Pr N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-29-1 p-Br-Ph H N n ⁱ Pr N ₃ F F IT n n XII-29-2 p-Br-Ph H N CH ₃ ⁱ Pr N ₃ F F IT n n XII-29-3 p-Br-Ph H n CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F IT n n XII-29-4 p-Br-Ph H n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F IT n n XII-29-5 p-Br-Ph H n CH ₂ Ph ⁱ Pr N ₃ F F IT n n XII-29-6 p-Br-Ph H n CH ₂ -indol-3-yl ⁱ Pr N ₃ F F IT n n XII-29-7 p-Br-Ph H n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F IT n n XII-29-8 p-Br-Ph * n * ⁱ Pr N ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-30-1 p-i-ph H N N ⁱ Pr N ₃ F F IT n n XII-30-2 p-i-ph H H CH ₃ ⁱ Pr N ₃ F F IT n n XII-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F IT n n XII-30-4 p-i-ph H n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F F IT n n XII-30-5 p-i-ph H n CH ₂ Ph ⁱ Pr N ₃ F F IT n n XII-30-6 p-i-ph H n CH ₂ -indol-3-yl ⁱ Pr N ₃ F F IT n n XII-30-7 p-i-ph H n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F F IT n n XII-30-8 p-i-ph * n * ⁱ Pr N ₃ F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-31-1 CH ₃ N N N ⁿ Bu N ₃ F F OH H H XII-31-2 CH ₃ N N CH ₃ ⁿ Bu N ₃ F F OH H H XII-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-31-8 CH ₃ * n * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-32-1 Et H H H ⁿ Bu N ₃ F F OH H H XII-32-2 Et H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-32-5 Et H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-32-8 Et * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-33-1 ⁱ Pr H H H ⁿ Bu N ₃ F F OH H H XII-33-2 ⁱ Pr H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-33-6 ⁱ Pr H H CH ₂ -ind ol-3-yl ⁿ Bu N ₃ F F OH H H XII-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-33-8 ⁱ Pr * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-34-1 ^t Bu H H N ⁿ Bu N ₃ F F OH H H XII-34-2 ^t Bu H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-34-8 ^t Bu * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XH-35-1 Ph H H H ⁿ Bu N ₃ F F OH H H XII-35-2 Ph H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-35-5 Ph H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-35-8 Ph * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-36-1 p-me-ph H H H ⁿ Bu N ₃ F F OH H H XII-36-2 p-me-ph H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-36-8 p-me-ph * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-37-1 p-f-ph H H H ⁿ Bu N ₃ F F OH H H XII-37-2 p-f-ph H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-37-8 p-f-ph * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-38-1 p-Cl-Ph H H H ⁿ Bu N ₃ F F OH H H XII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-38-8 p-Cl-Ph * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-39-1 p-Br-Ph H H H ⁿ Bu N ₃ F F OH H H XII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu N ₃ F F OH H H XII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-39-8 p-Br-Ph * H * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-40-1 p-1-ph N N n ⁿ Bu N ₃ F F OH H H XII-40-2 p-1-ph N N CH ₃ ⁿ Bu N ₃ F F OH H H XII-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F F OH H H XII-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu N ₃ F F OH H H XII-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu N ₃ F F OH H H XII-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F F OH H H XII-40-8 p-1-ph * n * ⁿ Bu N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-41-1 CH ₃ N N n Bz N ₃ F F OH H H XII-41-2 CH ₃ N N CH ₃ Bz N ₃ F F OH H H XII-41-3 CH ₃ n N CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-41-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-41-5 CH ₃ n n CH ₂ Ph Bz N ₃ F F OH H H XII-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-41-8 CH ₃ * n * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-42-1 Et H H H Bz N ₃ F F OH H H XII-42-2 Et H H CH ₃ Bz N ₃ F F OH H H XII-42-3 Et H H CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-42-5 Et H H CH ₂ Ph Bz N ₃ F F OH H H XII-42-6 Et H H CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-42-8 Et * H * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-43-1 ⁱ Pr N n n Bz N ₃ F F OH H H XII-43-2 ⁱ Pr N n CH ₃ Bz N ₃ F F OH H H XII-43-3 fpr N n CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-43-5 ⁱ Pr n n CH ₂ Ph Bz N ₃ F F OH H H XII-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-43-8 ⁱ Pr * n * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-44-1 ^t bu N N N Bz N ₃ F F OH H H XII-44-2 ^t bu N N CH ₃ Bz N ₃ F F OH H H XII-44-3 ^t bu N N CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-44-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-44-5 ^t bu n N CH ₂ Ph Bz N ₃ F F OH H H XII-44-6 ^t bu n N CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-44-7 ^t bu n n CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-44-8 ^t bu * n * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-45-1 Ph H H H Bz N ₃ F F OH H H XII-45-2 Ph H H CH ₃ Bz N ₃ F F OH H H XII-45-3 Ph H H CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-45-5 Ph H H CH ₂ Ph Bz N ₃ F F OH H H XII-45-6 Ph H H CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-45-8 Ph * H * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-46-1 p-me-ph H H H Bz N ₃ F F OH H H XII-46-2 p-me-ph H H CH ₃ Bz N ₃ F F OH H H XII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-46-5 p-me-ph H H CH ₂ Ph Bz N ₃ F F OH H H XII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-46-8 p-me-ph * H * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-47-1 p-f-ph H H H Bz N ₃ F F OH H H XII-47-2 p-f-ph H H CH ₃ Bz N ₃ F F OH H H XII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-47-5 p-f-ph H H CH ₂ Ph Bz N ₃ F F OH H H XII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-47-8 p-f-ph * H * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-48-1 p-Cl-Ph H H H Bz N ₃ F F OH H H XII-48-2 p-Cl-Ph H H CH ₃ Bz N ₃ F F OH H H XII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-48-5 p-Cl-Ph H H CH ₂ Ph Bz N ₃ F F OH H H XII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-48-8 p-Cl-Ph * H * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-49-1 p-Br-Ph H H H Bz N ₃ F F OH H H XII-49-2 p-Br-Ph H H CH ₃ Bz N ₃ F F OH H H XII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-49-5 p-Br-Ph H H CH ₂ Ph Bz N ₃ F F OH H H XII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-49-8 p-Br-Ph * H * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XII-50-1 p-1-ph N N n Bz N ₃ F F OH H H XII-50-2 p-1-ph N N CH ₃ Bz N ₃ F F OH H H XII-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F F OH H H XII-50-5 p-1-ph N n CH ₂ Ph Bz N ₃ F F OH H H XII-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz N ₃ F F OH H H XII-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz N ₃ F F OH H H XII-50-8 p-1-ph * n * Bz N ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-1-1 CH ₃ N n n CH ₃ N ₃ N F IT N N XIII-1-2 CH ₃ N n CH ₃ CH ₃ N ₃ N F IT N N XIII-1-3 CH ₃ n n CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-1-5 CH ₃ n n CH ₂ Ph CH ₃ N ₃ N F IT N N XIII-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ N ₃ N F IT N N XIII-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ N F IT N N XIII-1-8 CH ₃ * n * CH ₃ N ₃ N F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-2-1 Et H H H CH ₃ N ₃ N F IT N N XIII-2-2 Et H H CH ₃ CH ₃ N ₃ N F IT N N XIII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-2-5 Et H H CH ₂ Ph CH ₃ N ₃ N F IT N N XIII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N ₃ N F IT N N XIII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ N F IT N N XIII-2-8 Et * H * CH ₃ N ₃ N F IT n N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-3-1 ⁱ Pr N N N CH ₃ N ₃ N F IT N N XIII-3-2 ⁱ Pr N N CH ₃ CH ₃ N ₃ N F IT N N XIII-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N n XIII-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N n XIII-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ N ₃ N F IT N n XIII-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ N ₃ N F IT N n XIII-3-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ N F IT N n XIII-3-8 ⁱ Pr * N * CH ₃ N ₃ N F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-4-1 ^t bu N n n CH ₃ N ₃ N F it n n XIII-4-2 ^t bu N n CH ₃ CH ₃ N ₃ N F IT n n XIII-4-3 ^t bu N n CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT n n XIII-4-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT n n XIII-4-5 ^t bu N n CH ₂ Ph CH ₃ N ₃ N F IT n n XIII-4-6 ^t bu N n CH ₂ -indol-3-yl CH ₃ N ₃ n F IT n n XIII-4-7 ^t bu n n CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ n F IT n n XIII-4-8 ^t bu * n * CH ₃ N ₃ n F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-5-1 Ph H H H CH ₃ N ₃ H F OH H H XIII-5-2 Ph H H CH ₃ CH ₃ N ₃ H F OH H H XIII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ H F OH H H XIII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ H F OH H H XIII-5-5 Ph H H CH ₂ Ph CH ₃ N ₃ H F OH H H XIII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ H F OH H H XIII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ H F OH H H XIII-5-8 Ph * H * CH ₃ N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-6-1 p-me-ph H H H CH ₃ N ₃ H F OH H H XIII-6-2 p-me-ph H H CH ₃ CH ₃ N ₃ H F OH H H XIII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ H F OH H H XIII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ H F OH H H XIII-6-5 p-me-ph H H CH ₂ Ph CH ₃ N ₃ H F OH H H XIII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ H F OH H H XIII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ H F OH H H XIII-6-8 p-me-ph * H * CH ₃ N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-7-1 p-f-ph H H H CH ₃ N ₃ H F OH H H XIII-7-2 p-f-ph H H CH ₃ CH ₃ N ₃ H F OH H H XIII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ H F OH H H XIII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ H F OH H H XIII-7-6 p-f-ph H H CH ₂ Ph CH ₃ N ₃ H F OH H H XIII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ H F OH H H XIII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ H F OH H H XIII-7-20 p-f-ph * H * CH ₃ N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-8-1 p-Cl-Ph H H H CH ₃ N ₃ N F IT N n XIII-8-2 p-Cl-Ph H H CH ₃ CH ₃ N ₃ N F IT N n XIII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N n XIII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N n XIII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N ₃ N F IT N n XIII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ N F IT N n XIII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ N F IT N n XIII-8-8 p-Cl-Ph * H * CH ₃ N ₃ N F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-9-1 p-Br-Ph H H H CH ₃ N ₃ N F IT N N XIII-9-2 p-Br-Ph H H CH ₃ CH ₃ N ₃ N F IT N N XIII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N ₃ N F IT N N XIII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ N F IT N N XIII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ N F IT N N XIII-9-20 p-Br-Ph * H * CH ₃ N ₃ N F IT n N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-10-1 p-1-ph N N n CH ₃ N ₃ N F IT N N XIII-10-2 p-1-ph N N CH ₃ CH ₃ N ₃ N F IT N N XIII-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ N F IT N N XIII-10-5 p-1-ph N n CH ₂ Ph CH ₃ N ₃ N F IT N N XIII-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ N ₃ N F IT N N XIII-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ N F IT N N XIII-10-8 p-1-ph * n * CH ₃ N ₃ N F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-ll-l CH ₃ N n n Et N ₃ H F OH H H XSh-11-2 CH ₃ N n CH ₃ Et N ₃ H F OH H H XIII-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-11-5 CH ₃ N n CH ₂ Ph Et N ₃ H F OH H H XIII-11-6 CH ₃ N n CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-11-8 CH ₃ * n Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-12-1 Et H H H Et N ₃ H F OH H H XIII-12-2 Et H H CH ₃ Et N ₃ H F OH H H XIII-12-3 Et H H CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-12-5 Et H H CH ₂ Ph Et N ₃ H F OH H H XIII-12-6 Et H H CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-12-8 Et * H * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-13-1 ⁱ Pr N N n Et N ₃ H F OH H H XIII-13-2 ⁱ Pr N N CH ₃ Et N ₃ H F OH H H XIII-13-3 ⁱ Pr N n CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-13-5 ⁱ Pr N n CH ₂ Ph Et N ₃ H F OH H H XIII-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-13-8 ⁱ Pr * n * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-14-1 ^t bu N N N Et N ₃ H F OH H H XIII-14-2 ^t bu N N CH ₃ Et N ₃ H F OH H H XIII-14-3 ^t bu N N CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-14-4 ^t bu N N CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-14-5 ^t bu N N CH ₂ Ph Et N ₃ H F OH H H XIII-14-6 ^t bu N N CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-14-7 ^t bu n N CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-14-8 ^t bu * N * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-15-1 Ph H H H Et N ₃ H F OH H H XIII-15-2 Ph H H CH ₃ Et N ₃ H F OH H H XIII-15-3 Ph H H CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-15-5 Ph H H CH ₂ Ph Et N ₃ H F OH H H XIII-15-6 Ph H H CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-15-8 Ph * H * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-16-1 p-me-ph H H H Et N ₃ H F OH H H XIII-16-2 p-me-ph H H CH ₃ Et N ₃ H F OH H H XIII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-16-5 p-me-ph H H CH ₂ Ph Et N ₃ H F OH H H XIII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-16-8 p-me-ph * H * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-17-1 p-f-ph H H H Et N ₃ H F OH H H XIII-17-2 p-f-ph H H CH ₃ Et N ₃ H F OH H H XIII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-17-5 p-f-ph H H CH ₂ Ph Et N ₃ H F OH H H XIII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-17-8 p-f-ph * H * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-18-1 p-Cl-Ph H H H Et N ₃ H F OH H H XIII-18-2 p-Cl-Ph H H CH ₃ Et N ₃ H F OH H H XIII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-18-4 p-CI-Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-18-5 p-Cl-Ph H H CH ₂ Ph Et N ₃ H F OH H H XIII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-18-8 p-Cl-Ph * H * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-19-1 p-Br-Ph H H H Et N ₃ H F OH H H XIII-19-2 p-Br-Ph H H CH ₃ Et N ₃ H F OH H H XIII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-19-5 p-Br-Ph H H CH ₂ Ph Et N ₃ H F OH H H XIII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-19-8 p-Br-Ph * H * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-20-1 p-1-ph N N n Et N ₃ H F OH H H XIII-20-2 p-1-ph N N CH ₃ Et N ₃ H F OH H H XIII-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ H F OH H H XIII-20-5 p-1-ph N n CH ₂ Ph Et N ₃ H F OH H H XIII-20-6 p-1-ph N n CH ₂ -indol-3-yl Et N ₃ H F OH H H XIII-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et N ₃ H F OH H H XIII-20-8 p-1-ph * n * Et N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-21-1 CH ₃ N N n ⁱ Pr N ₃ N F IT N N XIII-21-2 CH ₃ N N CH ₃ ⁱ Pr N ₃ N F IT N N XIII-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N ₃ N F IT N n XIII-21-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ N F IT N n XIII-21-5 CH ₃ n n CH ₂ Ph ⁱ Pr N ₃ n F IT N n XIII-21-6 CH ₃ n n CH ₂ -indol-3-yl ⁱ Pr N ₃ n F IT N n XIII-21-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ n F IT N n XIII-21-8 CH ₃ n * ⁱ Pr N ₃ n F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-22-1 Et H H H ⁱ Pr N ₃ H F OH H H XIII-22-2 Et H H CH ₃ ⁱ Pr N ₃ H F OH H H XIII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N H F OH H H XIII-22-5 Et H H CH ₂ Ph ⁱ Pr N ₃ H F OH H H XIII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr N ₃ H F OH H H XIII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ H F OH H H XIII-22-8 Et * H * ⁱ Pr N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-23-1 ⁱ Pr N n n ⁱ Pr N ₃ N F IT N N XIII-23-2 ⁱ Pr N n CH ₃ ⁱ Pr N ₃ n F IT N N XIII-23-3 ⁱ Pr n n CH (CH ₃ ) ₂ ⁱ Pr N ₃ n F IT N N XIII-23-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ n F IT N N XIII-23-5 ⁱ Pr n n CH ₂ Ph ⁱ Pr N ₃ n F IT N N XIII-23-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr N ₃ n F IT N N XIII-23-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ n F IT N n XIII-23-8 ⁱ Pr * n * ⁱ Pr N ₃ n F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-24-1 ^t bu N N n ⁱ Pr N ₃ N F it N n XIII-24-2 ^t bu N N CH ₃ ⁱ Pr N ₃ N F IT N n XIII-24-3 ^t bu N n CH (CH ₃ ) ₂ ⁱ Pr N ₃ n F IT n n XIII-24-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ n F IT n n XIII-24-5 ^t bu N n CH ₂ Ph ⁱ Pr N ₃ n F IT n n XIII-24-6 ^t bu N n CH ₂ -indol-3-yl ⁱ Pr N ₃ n F IT n n XIII-24-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ n F IT n n XIII-24-8 ^t bu * n * ⁱ Pr N ₃ n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-25-1 Ph H H H ⁱ Pr N ₃ H F OH H H XIII-25-2 Ph H H CH ₃ ⁱ Pr N ₃ H F OH H H XIII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-25-5 Ph H H CH ₂ Ph ⁱ Pr N ₃ H F OH H H XIII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ H F OH H H XIII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ H F OH H H XIII-25-8 Ph * H * ⁱ Pr N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-26-1 p-me-ph H H H ⁱ Pr N ₃ H F OH H H XIII-26-2 p-me-ph H H CH ₃ ⁱ Pr N ₃ H F OH H H XIII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr N ₃ H F OH H H XIII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ H F OH H H XIII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ H F OH H H XIII-26-8 p-me-ph * H * ⁱ Pr N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-27-1 p-f-ph H H H ⁱ Pr N ₃ H F OH H H XIII-27-2 p-f-ph H H CH ₃ ⁱ Pr N ₃ H F OH H H XIII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr N ₃ H F OH H H XIII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ H F OH H H XIII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ H F OH H H XIII-27-8 p-f-ph H * ⁱ Pr N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-28-1 p-Cl-Ph H H H ⁱ Pr N ₃ H F OH H H XIII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr N ₃ H F OH H H XIII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr N ₃ H F OH H H XIII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ H F OH H H XIII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ H F OH H H XIII-28-8 p-Cl-Ph H * ⁱ Pr N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-29-1 p-Br-Ph H H H ⁱ Pr N ₃ H F OH H H XIII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr N ₃ H F OH H H XIII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ H F OH H H XIII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr N ₃ H F OH H H XIII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ H F OH H H XIII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ H F OH H H XIII-29-8 p-Br-Ph * H * ⁱ Pr N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-30-1 p-1-ph N N n ⁱ Pr N ₃ N F IT n N XIII-30-2 p-1-ph N N CH ₃ ⁱ Pr N ₃ N F IT n N XIII-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr N ₃ N F IT n n XIII-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ N F IT n n XIII-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr N ₃ N F IT n n XIII-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr N ₃ n F IT n n XIII-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ n F it n n XIII-30-8 p-1-ph * n ⁱ Pr N ₃ n F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-31-1 CH ₃ N N n ⁿ Bu N ₃ H F OH H H XIII-31-2 CH ₃ N N CH ₃ ⁿ Bu N ₃ H F OH H H XIII-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-31-6 CH ₃ n n CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-31-8 CH ₃ * n * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-32-1 Et H H H ⁿ Bu N ₃ H F OH H H XIII-32-2 Et H H CH ₃ ⁿ Bu N ₃ H F OH H H XIII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-32-5 Et H H CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-32-8 Et H * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-33-1 ⁱ Pr N N n ⁿ Bu N ₃ H F OH H H XIII-33-2 ⁱ Pr N N sun ₃ ⁿ Bu N ₃ H F OH H H XIII-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-33-5 ⁱ Pr N n CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-33-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-33-8 ⁱ Pr * n * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-34-1 ^t bu N N n ⁿ Bu N ₃ H F OH H H XIII-34-2 ^t bu N N sun ₃ ⁿ Bu N ₃ H F OH H H XIII-34-3 ^t bu N n CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-34-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-34-5 ^t bu N n CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-34-6 ^t bu N n CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-34-7 ^t bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-34-8 ^t bu * n * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-35-1 Ph H H H ⁿ Bu N ₃ H F OH H H XIII-35-2 Ph H H CH ₃ ⁿ Bu N ₃ H F OH H H XIII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-35-5 Ph H H CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-35-8 Ph * H * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-36-1 p-me-ph H H H ⁿ Bu N ₃ H F OH H H XIII-36-2 p-me-ph H H CH ₃ ⁿ Bu N ₃ H F OH H H XIII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-36-8 p-me-ph H * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-37-1 p-f-ph H H H ⁿ Bu N ₃ H F OH H H XIII-37-2 p-f-ph H H CH ₃ ⁿ Bu N ₃ H F OH H H XIII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-37-8 p-f-ph * H * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-38-1 p-Cl-Ph H H H ⁿ Bu N ₃ H F OH H H XIII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu N ₃ H F OH H H XIII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-38-8 p-Cl-Ph * H * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-39-1 p-Br-Ph H H H ⁿ Bu N ₃ H F OH H H XIII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu N ₃ H F OH H H XIII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-39-8 p-Br-Ph * H * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-40-1 p-1-ph N n n ⁿ Bu N ₃ H F OH H H XIII-40-2 p-1-ph N n CH ₃ ⁿ Bu N ₃ H F OH H H XIII-40-3 p-1-ph n n CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-40-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ H F OH H H XIII-40-5 p-1-ph n n CH ₂ Ph ⁿ Bu N ₃ H F OH H H XIII-40-6 p-1-ph n n CH ₂ -indol-3-yl ⁿ Bu N ₃ H F OH H H XIII-40-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ H F OH H H XIII-40-8 p-1-ph * n * ⁿ Bu N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-41-1 CH ₃ N N n Bz N ₃ H F OH H H XIII-41-2 CH ₃ N n CH ₃ Bz N ₃ H F OH H H XIII-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-41-5 CH ₃ N n CH ₂ Ph Bz N ₃ H F OH H H XIII-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-41-8 CH ₃ * n * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-42-1 Et H H H Bz N ₃ H F OH H H XIII-42-2 Et H H CH ₃ Bz N ₃ H F OH H H XIII-42-3 Et H H CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-42-5 Et H H CH ₂ Ph Bz N ₃ H F OH H H XIII-42-6 Et H H CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-42-8 Et * H * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XSh-43-1 ⁱ Pr N N n Bz N ₃ H F OH H H XIII-43-2 ⁱ Pr N N CH ₃ Bz N ₃ H F OH H H XIII-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-43-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-43-5 ⁱ Pr N n CH ₂ Ph Bz N ₃ H F OH H H XIII-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-43-8 ⁱ Pr * n Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-44-1 ^t Bu N N n Bz N ₃ H F OH H H XIII-44-2 ^t Bu N N CH ₃ Bz N ₃ H F OH H H XIII-44-3 ^t Bu N N CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-44-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-44-5 ^t Bu N n CH ₂ Ph Bz N ₃ H F OH H H XIII-44-6 ^t Bu N n CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-44-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-44-8 ^t Bu * n * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-45-1 Ph H H H Bz N ₃ H F OH H H XIII-45-2 Ph H H CH ₃ Bz N ₃ H F OH H H XIII-45-3 Ph H H CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-45-5 Ph H H CH ₂ Ph Bz N ₃ H F OH H H XIII-45-6 Ph H H CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-45-8 Ph * H * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-46-1 p-me-ph H H H Bz N ₃ H F OH H H XIII-46-2 p-me-ph H H CH ₃ Bz N ₃ H F OH H H XIII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-46-5 p-me-ph H H CH ₂ Ph Bz N ₃ H F OH H H XIII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-46-8 p-me-ph * H * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-47-1 p-f-ph H H H Bz N ₃ H F OH H H XIII-47-2 p-f-ph H H CH ₃ Bz N ₃ H F OH H H XIII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-47-5 p-f-ph H H CH ₂ Ph Bz N ₃ H F OH H H XIII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-47-8 p-f-ph * H * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-48-1 p-Cl-Ph H H H Bz N ₃ H F OH H H XIII-48-2 p-Cl-Ph H H CH ₃ Bz N ₃ H F OH H H XIII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-48-5 p-Cl-Ph H H CH ₂ Ph Bz N ₃ H F OH H H XIII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-48-8 p-Cl-Ph * H * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-49-1 p-Br-Ph H H H Bz N ₃ H F OH H H XIII-49-2 p-Br-Ph H H CH ₃ Bz N ₃ H F OH H H XIII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-49-5 p-Br-Ph H H CH ₂ Ph Bz N ₃ H F OH H H XIII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-49-8 p-Br-Ph * H Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIII-50-1 p-1-ph N N n Bz N ₃ H F OH H H XIII-50-2 p-1-ph N N CH ₃ Bz N ₃ H F OH H H XIII-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ H F OH H H XIII-50-5 p-1-ph N n CH ₂ Ph Bz N ₃ H F OH H H XIII-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz N ₃ H F OH H H XIII-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz N ₃ H F OH H H XIII-50-8 p-1-ph * n * Bz N ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

XTV-1 table. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-1-1 CH ₃ N n N CH ₃ N ₃ F N IT N N XIV-1-2 CH ₃ N n CH ₃ CH ₃ N ₃ F N IT N N XIV-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N N XIV-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N N XIV-1-5 CH ₃ N n CH ₂ Ph CH ₃ N ₃ F N IT N N XIV-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N ₃ F N IT N N XIV-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N IT N N XIV-1-8 CH ₃ * n * CH ₃ N ₃ F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-2-1 Et H H H CH ₃ N ₃ F N IT n n XIV-2-2 Et H H CH ₃ CH ₃ N ₃ F N IT n n XIV-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-2-5 Et H H CH ₂ Ph CH ₃ N ₃ F N it n n XIV-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N ₃ F N it n n XIV-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N it n n XIV-2-8 Et * H * CH ₃ N ₃ F N it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-3-1 ⁱ Pr H H H CH ₃ N ₃ F n IT n n XIV-3-2 ⁱ Pr H H CH ₃ CH ₃ N ₃ F n it n n XIV-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ N ₃ F n it n n XIV-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F n it n n XIV-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ N ₃ F n it n n XIV-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ N ₃ F n it n n XIV-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F n it n n XIV-3-8 ⁱ Pr * H * CH ₃ N ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-4-1 ^t Bu H H H CH ₃ N ₃ F N IT N n XIV-4-2 ^t Bu H H CH ₃ CH ₃ N ₃ F N IT N n XIV-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-4-5 ^t Bu H H CH ₂ Ph CH ₃ N ₃ F N IT n n XIV-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ N ₃ F N IT n n XIV-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N IT n n XIV-4-8 ^t Bu * H * CH ₃ N ₃ F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-5-1 Ph H H H CH ₃ N ₃ F N IT n n XIV-5-2 Ph H H CH ₃ CH ₃ N ₃ F N IT n n XIV-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-5-5 Ph H H CH ₂ Ph CH ₃ N ₃ F N IT n n XIV-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F N IT n n XIV-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N IT n n XIV-5-8 Ph * H * CH ₃ N ₃ F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-6-1 p-me-ph H H H CH ₃ N ₃ F N IT n n XIV-6-2 p-me-ph H H CH ₃ CH ₃ N ₃ F N IT n n XIV-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F n IT n n XIV-6-5 p-me-ph H H CH ₂ Ph CH ₃ N ₃ F n IT n n XIV-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F n IT n n XIV-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F n it n n XIV-6-8 p-me-ph H * .. CH ₃ N ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-7-1 p-f-ph H H H CH ₃ N ₃ F H OH H H XIV-7-2 p-f-ph H H CH ₃ CH ₃ N ₃ F H OH H H XIV-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F H OH H H XIV-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F H OH H H XIV-7-6 p-f-ph H H CH ₂ Ph CH ₃ N ₃ F H OH H H XIV-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F H OH H H XIV-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F H OH H H XIV-7-20 p-f-ph * H * CH ₃ N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-8-1 p-Cl-Ph H H H CH ₃ N ₃ F N IT N N XIV-8-2 p-Cl-Ph H H CH ₃ CH ₃ N ₃ F N IT N N XIV-8-3 p-CI-Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N N XIV-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT n n XIV-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N ₃ F N IT n n XIV-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F N IT n n XIV-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N IT n n XIV-8-8 p-Cl-Ph * H * CH ₃ N ₃ F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-9-1 p-Br-Ph H H H CH ₃ N ₃ F N IT N n XIV-9-2 p-Br-Ph H H CH ₃ CH ₃ N ₃ F N IT N n XIV-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N n XIV-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N n XIV-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N ₃ F N IT n n XIV-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N ₃ F N IT n n XIV-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N IT n n XIV-9-20 p-Br-Ph * H * CH ₃ N ₃ F N it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-10-1 p-1-ph n N N CH ₃ N ₃ F N IT N N XIV-10-2 p-1-ph n N CH ₃ CH ₃ N ₃ F N IT N N XIV-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N N XIV-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N ₃ F N IT N n XIV-10-5 p-1-ph n n CH ₂ Ph CH ₃ N ₃ F N IT N n XIV-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N ₃ F N IT N n XIV-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ N ₃ F N IT N n XIV-10-8 p-1-ph * n CH ₃ N ₃ F N IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-11-1 CH ₃ N N n Et N ₃ F H OH H H XIV-11-2 CH ₃ N N CH ₃ Et N ₃ F H OH H H XIV-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-11-5 CH ₃ N n CH ₂ Ph Et N ₃ F H OH H H XIV-11-6 CH ₃ N n CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-11-8 CH ₃ * n * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-12-1 Et H H H Et N ₃ F H OH H H XIV-12-2 Et H H CH ₃ Et N ₃ F H OH H H XIV-12-3 Et H H CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-12-5 Et H H CH ₂ Ph Et N ₃ F H OH H H XIV-12-6 Et H H CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-12-8 Et * H * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-13-1 ⁱ Pr N N n Et N ₃ F H OH H H XIV-13-2 ⁱ Pr N N CH ₃ Et N ₃ F H OH H H XIV-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-13-5 ⁱ Pr N n CH ₂ Ph Et N ₃ F H OH H H XIV-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-13-8 ⁱ Pr * n * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-14-1 ^t Bu N n n Et N ₃ F H OH H H XIV-14-2 ^t Bu N n CH ₃ Et N ₃ F H OH H H XIV-14-3 ^t Bu N n CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-14-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-14-5 ^t Bu N n CH ₂ Ph Et N ₃ F H OH H H XIV-14-6 ^t Bu N n CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-14-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-14-8 ^t Bu * n * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-15-1 Ph H H H Et N ₃ F H OH H H XIV-15-2 Ph H H CH ₃ Et N ₃ F H OH H H XIV-15-3 Ph H H CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-15-5 Ph H H CH ₂ Ph Et N ₃ F H OH H H XIV-15-6 Ph H H CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-15-8 Ph * H * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-16-1 p-me-ph H H H Et N ₃ F H OH H H XIV-16-2 p-me-ph H H CH ₃ Et N ₃ F H OH H H XIV-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-16-5 p-me-ph H H CH ₂ Ph Et N ₃ F H OH H H XIV-16-6 p-me-ph H H CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-16-8 p-me-ph * H * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-17-1 p-f-ph H H H Et N ₃ F H OH H H XIV-17-2 p-f-ph H H CH ₃ Et N ₃ F H OH H H XIV-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-17-5 p-f-ph H H CH ₂ Ph Et N ₃ F H OH H H XIV-17-6 p-f-ph H H CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-17-8 p-f-ph * H * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-18-1 p-Cl-Ph H H H Et N ₃ F H OH H H XIV-18-2 p-Cl-Ph H H CH ₃ Et N ₃ F H OH H H XIV-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-18-5 p-Cl-Ph H H CH ₂ Ph Et N ₃ F H OH H H XIV-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-18-8 p-Cl-Ph * H * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-19-1 p-Br-Ph H H H Et N ₃ F H OH H H XIV-19-2 p-Br-Ph H H CH ₃ Et N ₃ F H OH H H XIV-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-19-5 p-Br-Ph H H CH ₂ Ph Et N ₃ F H OH H H XIV-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-19-8 p-Br-Ph * H * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-20-1 p-1-ph N N n Et N ₃ F H OH H H XIV-20-2 p-1-ph N N CH ₃ Et N ₃ F H OH H H XIV-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et N ₃ F H OH H H XIV-20-5 p-1-ph N n CH ₂ Ph Et N ₃ F H OH H H XIV-20-6 p-1-ph N n CH ₂ -indol-3-yl Et N ₃ F H OH H H XIV-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et N ₃ F H OH H H XIV-20-8 p-1-ph * n * Et N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-21-1 CH ₃ N N n ⁱ Pr N ₃ F n IT n n XIV-21-2 CH ₃ N N CH ₃ ⁱ Pr N ₃ F n IT n n XIV-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N ₃ F n it n n XIV-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F n it n n XIV-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N ₃ F n it n n XIV-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N ₃ F n it n n XIV-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F n it n n XIV-21-8 CH ₃ * n * ⁱ Pr N ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-22-1 Et H H H ⁱ Pr N ₃ F H OH H H XIV-22-2 Et H H CH ₃ ⁱ Pr N ₃ F H OH H H XIV-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-22-5 Et H H CH ₂ Ph ⁱ Pr N ₃ F H OH H H XIV-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F H OH H H XIV-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F H OH H H XIV-22-8 Et * H * ⁱ Pr N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-23-1 ⁱ Pr N N N ^t Bu N ₃ F N IT N N XIV-23-2 ⁱ Pr N N CH ₃ ^t Bu N ₃ F N IT N N XIV-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ^t Bu N ₃ F N IT N N XIV-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ^t Bu N ₃ F N IT N N XIV-23-5 ⁱ Pr N N CH ₂ Ph ^t Bu N ₃ F N IT N N XIV-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ^t Bu N ₃ F N IT N N XIV-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ^t Bu N ₃ F N IT N N XIV-23-8 ⁱ Pr * N * ^t Bu N ₃ F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-24-1 ^t Bu H H H ⁱ Pr N ₃ F H OH H H XIV-24-2 ^t Bu H H CH ₃ ⁱ Pr N ₃ F H OH H H XIV-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr N ₃ F H OH H H XIV-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F H OH H H XIV-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F H OH H H XIV-24-8 ^t Bu * H * ⁱ Pr N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-25-1 Ph H H H ⁱ Pr N ₃ F N IT n n XIV-25-2 Ph H H CH ₃ ⁱ Pr N ₃ F n IT n n XIV-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F n it n n XIV-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F n it n n XIV-25-5 Ph H H CH ₂ Ph ⁱ Pr N ₃ F n it n n XIV-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F n it n n XIV-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F n it n n XIV-25-8 Ph * H * ⁱ Pr N ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-26-1 p-me-ph H H H ⁱ Pr N ₃ F H OH H H XIV-26-2 p-me-ph H H CH ₃ ⁱ Pr N ₃ F H OH H H XIV-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr N ₃ F H OH H H XIV-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F H OH H H XIV-26.7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F H OH H H XIV-26-8 p-me-ph * H * ⁱ Pr N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-27-1 p-f-ph H H H ⁱ Pr N ₃ F H OH H H XIV-27-2 p-f-ph H H CH ₃ ⁱ Pr N ₃ F H OH H H XIV-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr N ₃ F H OH H H XIV-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F H OH H H XIV-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F H OH H H XIV-27-8 p-f-ph * H * ⁱ Pr N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-28-1 p-Cl-Ph H H H ⁱ Pr N ₃ F H OH H H XIV-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr N ₃ F H OH H H XIV-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr N ₃ F H OH H H XIV-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F H OH H H XIV-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F H OH H H XIV-28-8 p-Cl-Ph * H * ⁱ Pr N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-29-1 p-Br-Ph H H H ⁱ Pr N ₃ F H OH H H XIV-29-2 p-Br-Ph H H CH ₃ ⁱ Pr N ₃ F H OH H H XIV-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F H OH H H XIV-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr N ₃ F H OH H H XIV-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr N ₃ F H OH H H XIV-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F H OH H H XIV-29-8 p-Br-Ph * H * ⁱ Pr N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-30-1 p-1-ph N N n ⁱ Pr N ₃ F n IT n n XIV-30-2 p-1-ph N N CH ₃ ⁱ Pr N ₃ F n it n n XIV-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr N ₃ F n it n n XIV-30-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N ₃ F n it n n XIV-30-5 p-1-ph N N CH ₂ Ph ⁱ Pr N ₃ F n it n n XIV-30-6 p-1-ph N N CH ₂ -indol-3-yl ⁱ Pr N ₃ F n it n n XIV-30-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N ₃ F n it n n XIV-30-8 p-1-ph * n * ⁱ Pr N ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-31-1 CH ₃ N n n ⁿ Bu N ₃ F H OH H H XIV-31-2 CH ₃ N n CH ₃ ⁿ Bu N ₃ F H OH H H XIV-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-31-8 CH ₃ * n * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-32-1 Et H H H ⁿ Bu N ₃ F H OH H H XIV-32-2 Et H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-32-5 Et H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-32-8 Et * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-33-1 ⁱ Pr H H H ⁿ Bu N ₃ F H OH H H XIV-33-2 ⁱ Pr H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-33-8 ⁱ Pr * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-34-1 ^t Bu N N N ⁿ Bu N ₃ F H OH H H XIV-34-2 ^t Bu N N sn3 ⁿ Bu N ₃ F H OH H H XIV-34-3 ^t Bu N N CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-34-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-34-5 ^t Bu N N CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-34-6 ^t Bu N N CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-34-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-34-8 ^t Bu * N * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-35-1 Ph H H H ⁿ Bu N ₃ F H OH H H XIV-35-2 Ph H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-35-5 Ph H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-35-8 Ph * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-36-1 p-me-ph H H H ⁿ Bu N ₃ F H OH H H XIV-36-2 p-me-ph H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-36-8 p-me-ph * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-37-1 p-f-ph H H H ⁿ Bu N ₃ F H OH H H XIV-37-2 p-f-ph H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-37-8 p-f-ph * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-38-1 p-Cl-Ph H H H ⁿ Bu N ₃ F H OH H H XIV-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-38-8 p-Cl-Ph * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-39-1 p-Br-Ph H H H ⁿ Bu N ₃ F H OH H H XIV-39-2 p-Br-Ph H H CH ₃ ⁿ Bu N ₃ F H OH H H XIV-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-39-8 p-Br-Ph * H * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-40-1 p-1-ph N N n ⁿ Bu N ₃ F H OH H H XIV-40-2 p-1-ph N N CH ₃ ⁿ Bu N ₃ F H OH H H XIV-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N ₃ F H OH H H XIV-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu N ₃ F H OH H H XIV-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu N ₃ F H OH H H XIV-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N ₃ F H OH H H XIV-40-8 p-1-ph * n * ⁿ Bu N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-41-1 CH ₃ N N n Bz N ₃ F H OH H H XIV-41-2 CH ₃ N N CH ₃ Bz N ₃ F H OH H H XIV-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-41-5 CH ₃ N n CH ₂ Ph Bz N ₃ F H OH H H XIV-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-41-8 CH ₃ * n * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-42-1 Et H H H Bz N ₃ F H OH H H XIV-42-2 Et H H CH ₃ Bz N ₃ F H OH H H XIV-42-3 Et H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-42-5 Et H H CH ₂ Ph Bz N ₃ F H OH H H XIV-42-6 Et H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-42-8 Et * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-43-1 ⁱ Pr N N N Bz N ₃ F H OH H H XIV-43-2 ⁱ Pr N N CH ₃ Bz N ₃ F H OH H H XIV-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-43-5 ⁱ Pr N n CH ₂ Ph Bz N ₃ F H OH H H XIV-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-43-8 ⁱ Pr * n * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-44-1 ^t Bu H H H Bz N ₃ F H OH H H XIV-44-2 ^t Bu H H CH ₃ Bz N ₃ F H OH H H XIV-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-44-5 ^t Bu H H CH ₂ Ph Bz N ₃ F H OH H H XIV-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-44-8 ^t Bu * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-45-1 Ph H H H Bz N ₃ F H OH H H XIV-45-2 Ph H H CH ₃ Bz N ₃ F H OH H H XIV-45-3 Ph H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-45-5 Ph H H CH ₂ Ph Bz N ₃ F H OH H H XIV-45-6 Ph H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-45-8 Ph * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-46-1 p-me-ph H H H Bz N ₃ F H OH H H XIV-46-2 p-me-ph H H CH ₃ Bz N ₃ F H OH H H XIV-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-46-5 p-me-ph H H CH ₂ Ph Bz N ₃ F H OH H H XIV-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-46-8 p-me-ph * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-47-1 p-f-ph H H H Bz N ₃ F H OH H H XIV-47-2 p-f-ph H H CH ₃ Bz N ₃ F H OH H H XIV-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-47-5 p-f-ph H H CH ₂ Ph Bz N ₃ F H OH H H XIV-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-47-8 p-f-ph * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-48-1 p-Cl-Ph H H H Bz N ₃ F H OH H H XIV-48-2 p-Cl-Ph H H CH ₃ Bz N ₃ F H OH H H XIV-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-48-5 p-Cl-Ph H H CH ₂ Ph Bz N ₃ F H OH H H XIV-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-48-8 p-Cl-Ph * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIV-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-49-1 p-Br-Ph H H H Bz N ₃ F H OH H H XIV-49-2 p-Br-Ph H H CH ₃ Bz N ₃ F H OH H H XIV-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-49-5 p-Br-Ph H H CH ₂ Ph Bz N ₃ F H OH H H XIV-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-49-8 p-Br-Ph * H * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIV-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIV-50-1 p-1-ph N N N Bz N ₃ F H OH H H XIV-50-2 p-1-ph N N CH ₃ Bz N ₃ F H OH H H XIV-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-50-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Bz N ₃ F H OH H H XIV-50-5 p-1-ph N N CH ₂ Ph Bz N ₃ F H OH H H XIV-50-6 p-1-ph N N CH ₂ -indol-3-yl Bz N ₃ F H OH H H XIV-50-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Bz N ₃ F H OH H H XIV-50-8 p-1-ph * N * Bz N ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-1-1 CH ₃ N N N CH ₃ F F N IT N N XV-1-2 CH ₃ N N CH ₃ CH ₃ F F N IT N N XV-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ F F N IT N N XV-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N IT N N XV-1-5 CH ₃ N N CH ₂ Ph CH ₃ F F N IT N N XV-1-6 CH ₃ N N CH ₂ -indol-3-yl CH ₃ F F N IT N N XV-1-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ CH ₃ F F N IT N N XV-1-8 CH ₃ N * CH ₃ F F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-2-1 Et H H H CH ₃ F F N IT n n XV-2-2 Et H H CH ₃ CH ₃ F F N IT n n XV-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ F F N it n n XV-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F n it n n XV-2-5 Et H H CH ₂ Ph CH ₃ F F n it n n XV-2-6 Et H H CH ₂ -indol-3-yl CH ₃ F F n it n n XV-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ F F n it n n XV-2-8 Et * H * CH ₃ F F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-3-1 ⁱ Pr N N n CH ₃ F F N IT N N XV-3-2 ⁱ Pr N N CH ₃ CH ₃ F F N IT N N XV-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ F F N IT N N XV-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N IT N N XV-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ F F N IT N N XV-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ F F N IT N N XV-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ F F N IT N N XV-3-8 ⁱ Pr * n * CH ₃ F F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-4-1 ^t Bu N n N CH ₃ F F N IT n n XV-4-2 ^t Bu N N CH ₃ CH ₃ F F N IT n n XV-4-3 ^t Bu N n CH (CH ₃ ) ₂ CH ₃ F F N IT n n XV-4-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N it n n XV-4-5 ^t Bu N n CH ₂ Ph CH ₃ F F N it n n XV-4-6 ^t Bu N n CH ₂ -indol-3-yl CH ₃ F F N it n n XV-4-7 ^t Bu n N CH ₂ CH ₂ SCH ₃ CH ₃ F F N it n n XV-4-8 ^t Bu * n * CH ₃ F F N it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-5-1 Ph H H H CH ₃ F F N IT n n XV-5-2 Ph H H CH ₃ CH ₃ F F N IT n n XV-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ F F n IT n n XV-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F n it n n XV-5-5 Ph H H CH ₂ Ph CH ₃ F F n it n n XV-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ F F n it n n XV-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F n it n n XV-5-8 Ph * H * CH ₃ F F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-6-1 p-me-ph H H H CH ₃ F F N IT N N XV-6-2 p-me-ph H H CH ₃ CH ₃ F F N IT N N XV-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ F F N IT n N XV-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N IT n N XV-6-5 p-me-ph H H CH ₂ Ph CH ₃ F F N IT n n XV-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ F F N IT n n XV-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F N IT n n XV-6-8 p-me-ph * H * CH ₃ F F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-7-1 p-f-ph H H H CH ₃ F F N IT n n XV-7-2 p-f-ph H H CH ₃ CH ₃ F F n IT n n XV-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ F F n it n n XV-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F n it n n XV-7-6 p-f-ph H H CH ₂ Ph CH ₃ F F n it n n XV-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ F F n it n n XV-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F n it n n XV-7-20 p-f-ph * H * CH ₃ F F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-8-1 p-Cl-Ph H H H CH ₃ F F N IT N N XV-8-2 p-Cl-Ph H H CH ₃ CH ₃ F F N IT n N XV-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ F F N IT n N XV-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N IT n n XV-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ F F N IT n n XV-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ F F N IT n n XV-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F N IT n n XV-8-8 p-Cl-Ph * H * CH ₃ F F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-9-1 p-Br-Ph H H H CH ₃ F F N IT N n XV-9-2 p-Br-Ph H H CH ₃ CH ₃ F F N IT N n XV-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ F F N IT N n XV-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N IT N n XV-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ F F N IT N n XV-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ F F N IT N n XV-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F N IT n n XV-9-20 p-Br-Ph * H * CH ₃ F F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-10-1 p-1-ph n N n CH ₃ F F N IT N N XV-10-2 p-1-ph N N CH ₃ CH ₃ F F N IT N N XV-10-3 p-1-ph n N CH (CH ₃ ) ₂ CH ₃ F F N IT N N XV-10-4 p-1-ph n N CH ₂ CH (CH ₃ ) ₂ CH ₃ F F N IT N N XV-10-5 p-1-ph n N CH ₂ Ph CH ₃ F F N IT N N XV-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ F F N IT N N XV-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ F F N IT N N XV-10-8 p-1-ph * n * CH ₃ F F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-11-1 CH ₃ N N n Et F F H OH H H XV-11-2 CH ₃ N N CH ₃ Et F F H OH H H XV-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et F F H OH H H XV-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-11-5 CH ₃ N n CH ₂ Ph Et F F H OH H H XV-11-6 CH ₃ N n CH ₂ -indol-3-yl Et F F H OH H H XV-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-11-8 CH ₃ * n * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-12-1 Et H H H Et F F H OH H H XV-12-2 Et H H CH ₃ Et F F H OH H H XV-12-3 Et H H CH (CH ₃ ) ₂ Et F F H OH H H XV-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-12-5 Et H H CH ₂ Ph Et F F H OH H H XV-12-6 Et H H CH ₂ -indol-3-yl Et F F H OH H H XV-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-12-8 Et * H * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-13-1 ⁱ Pr N N n Et F F H OH H H XV-13-2 ⁱ Pr N N CH ₃ Et F F H OH H H XV-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et F F H OH H H XV-13-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-13-5 ⁱ Pr N N CH ₂ Ph Et F F H OH H H XV-13-6 ⁱ Pr N N CH ₂ -indol-3-yl Et F F H OH H H XV-13-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-13-8 ⁱ Pr * n * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-14-1 ^t Bu N n n Et F F H OH H H XV-14-2 ^t Bu N n CH ₃ Et F F H OH H H XV-14-3 ^t Bu n n CH (CH ₃ ) ₂ Et F F H OH H H XV-14-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-14-5 ^t Bu n n CH ₂ Ph Et F F H OH H H XV-14-6 ^t Bu n n CH ₂ -indol-3-yl Et F F H OH H H XV-14-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-14-8 ^t Bu * n * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-15-1 Ph H H H Et F F H OH H H XV-15-2 Ph H H CH ₃ Et F F H OH H H XV-15-3 Ph H H CH (CH ₃ ) ₂ Et F F H OH H H XV-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-15-5 Ph H H CH ₂ Ph Et F F H OH H H XV-15-6 Ph H H CH ₂ -indol-3-yl Et F F H OH H H XV-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-15-8 Ph * H * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-16-1 p-me-ph H H H Et F F H OH H H XV-16-2 p-me-ph H H CH ₃ Et F F H OH H H XV-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et F F H OH H H XV-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-16-5 p-me-ph H H CH ₂ Ph Et F F H OH H H XV-16-6 p-me-ph H H CH ₂ -indol-3-yl Et F F H OH H H XV-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-16-8 p-me-ph * H * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-17-1 p-f-ph H H H Et F F H OH H H XV-17-2 p-f-ph H H CH ₃ Et F F H OH H H XV-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et F F H OH H H XV-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-17-5 p-f-ph H H CH ₂ Ph Et F F H OH H H XV-17-6 p-f-ph H H CH ₂ -indol-3-yl Et F F H OH H H XV-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-17-8 p-f-ph * H * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-18-1 p-Cl-Ph H H H Et F F H OH H H XV-18-2 p-Cl-Ph H H CH ₃ Et F F H OH H H XV-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et F F H OH H H XV-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-18-S p-Cl-Ph H H CH ₂ Ph Et F F H OH H H XV-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et F F H OH H H XV-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-18-8 p-Cl-Ph * H * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-19-1 p-Br-Ph H H H Et F F H OH H H XV-19-2 p-Br-Ph H H CH ₃ Et F F H OH H H XV-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et F F H OH H H XV-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-19-5 p-Br-Ph H H CH ₂ Ph Et F F H OH H H XV-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et F F H OH H H XV-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-19-8 p-Br-Ph * H * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-20-1 p-1-ph N n n Et F F H OH H H XV-20-2 p-1-ph N n CH ₃ Et F F H OH H H XV-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et F F H OH H H XV-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et F F H OH H H XV-20-5 p-1-ph N n CH ₂ Ph Et F F H OH H H XV-20-6 p-1-ph n n CH ₂ -indol-3-yl Et F F H OH H H XV-20-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Et F F H OH H H XV-20-8 p-1-ph * n * Et F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-21-1 CH ₃ N n n ⁱ Pr F F N IT n n XV-21-2 CH ₃ N n CH ₃ ⁱ Pr F F N IT n n XV-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr F F N IT n n XV-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F N it n n XV-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr F F N it n n XV-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr F F N it n n XV-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr F F N it n n XV-21-8 CH ₃ * n * ⁱ Pr F F N it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-22-1 Et H H H ⁱ Pr F F H OH H H XV-22-2 Et H H CH ₃ ⁱ Pr F F H OH H H XV-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-22-5 Et H H CH ₂ Ph ⁱ Pr F F H OH H H XV-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-22-8 Et * H * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-23-1 ⁱ Pr N N N ⁱ Pr F F H OH H H XV-23-2 ⁱ Pr N N CH ₃ ⁱ Pr F F H OH H H XV-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr F F H OH H H XV-23-6 ⁱ Pr n N CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-23-7 ⁱ Pr n N CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-23-8 ⁱ Pr * N * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-24-1 ^t Bu N N n ⁱ Pr F F N IT N N XV-24-2 ^t Bu N N CH ₃ ⁱ Pr F F N IT N N XV-24-3 ^t Bu N N CH (CH ₃ ) ₂ ⁱ Pr F F N IT N N XV-24-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F N IT N N XV-24-5 ^t Bu N N CH ₂ Ph ⁱ Pr F F N IT n n XV-24-6 ^t Bu N N CH ₂ -indol-3-yl ⁱ Pr F F N IT n n XV-24-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ ⁱ Pr F F N IT n n XV-24-8 ^t Bu * N * ⁱ Pr F F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-25-1 Ph H H H ⁱ Pr F F H OH H H XV-25-2 Ph H H CH ₃ ⁱ Pr F F H OH H H XV-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-25-5 Ph H H CH ₂ Ph ⁱ Pr F F H OH H H XV-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-25-8 Ph * H * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-26-1 p-me-ph H H H ⁱ Pr F F H OH H H XV-26-2 p-me-ph H H CH ₃ ⁱ Pr F F H OH H H XV-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr F F H OH H H XV-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-26-8 p-me-ph * H * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-27-1 p-f-ph H H H ⁱ Pr F F H OH H H XV-27-2 p-f-ph H H CH ₃ ⁱ Pr F F H OH H H XV-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr F F H OH H H XV-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-27-8 p-f-ph * H * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-28-1 p-Cl-Ph H H H ⁱ Pr F F H OH H H XV-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr F F H OH H H XV-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-28-5 p-Cl-Ph H H Chzph ⁱ Pr F F H OH H H XV-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-28-8 p-Cl-Ph * H * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-29-1 p-Br-Ph H H H ⁱ Pr F F H OH H H XV-29-2 p-Br-Ph H H CH ₃ ⁱ Pr F F H OH H H XV-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F H OH H H XV-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr F F H OH H H XV-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr F F H OH H H XV-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F H OH H H XV-29-8 p-Br-Ph * H * ⁱ Pr F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-30-1 p-1-ph N N n ⁱ Pr F F N IT N N XV-30-2 p-1-ph N N sn3 ⁱ Pr F F N IT N N XV-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr F F N IT N N XV-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F N IT N N XV-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr F F N IT N N XV-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr F F N IT N N XV-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr F F N IT N N XV-30-8 p-1-ph * n * ⁱ Pr F F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-31-1 CH ₃ N N N ⁿ Bu F F H OH H H XV-31-2 CH ₃ N N CH ₃ ⁿ Bu F F H OH H H XV-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu F F H OH H H XV-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-31-8 CH ₃ * N * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-32-1 Et H H H ⁿ Bu F F H OH H H XV-32-2 Et H H CH ₃ ⁿ Bu F F H OH H H XV-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-32-5 Et H H CH ₂ Ph ⁿ Bu F F H OH H H XV-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-32-8 Et * H * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-33-1 ⁱ Pr N N N ⁿ Bu F F H OH H H XV-33-2 ⁱ Pr N N CH ₃ ⁿ Bu F F H OH H H XV-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-33-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu F F H OH H H XV-33-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-33-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-33-8 ⁱ Pr * N * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-34-1 ^t Bu N n n ⁿ Bu F F n IT n n XV-34-2 ^t Bu N n CH ₃ ⁿ Bu F F n IT n n XV-34-3 ^t Bu N n CH (CH ₃ ) ₂ ⁿ Bu F F n it n n XV-34-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F n it n n XV-34-5 ^t Bu n n CH ₂ Ph ⁿ Bu F F n it n n XV-34-6 ^t Bu n n CH ₂ -indol-3-yl ⁿ Bu F F n it n n XV-34-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ ⁿ Bu F F n it n n XV-34-8 ^t Bu * n * ⁿ Bu F F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-35-1 Ph H H H ⁿ Bu F F H OH H H XV-35-2 Ph H H CH ₃ ⁿ Bu F F H OH H H XV-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-35-5 Ph H H CH ₂ Ph ⁿ Bu F F H OH H H XV-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-35-8 Ph * H * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-36-1 p-me-ph H H H ⁿ Bu F F H OH H H XV-36-2 p-me-ph H H CH ₃ ⁿ Bu F F H OH H H XV-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu F F H OH H H XV-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-36-8 p-me-ph * H * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-37-1 p-f-ph H H H ⁿ Bu F F H OH H H XV-37-2 p-f-ph H H CH ₃ ⁿ Bu F F H OH H H XV-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu F F H OH H H XV-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-37-8 p-f-ph * H * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-38-1 p-Cl-Ph H H H ⁿ Bu F F H OH H H XV-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu F F H OH H H XV-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu F F H OH H H XV-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-38-8 p-Cl-Ph * H * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-39-1 p-Br-Ph H H H ⁿ Bu F F H OH H H XV-39-2 p-Br-Ph H H CH ₃ ⁿ Bu F F H OH H H XV-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu F F H OH H H XV-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-39-8 p-Br-Ph * H * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-40-1 p-1-ph N N n ⁿ Bu F F H OH H H XV-40-2 p-1-ph N N CH ₃ ⁿ Bu F F H OH H H XV-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F H OH H H XV-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu F F H OH H H XV-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu F F H OH H H XV-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu F F H OH H H XV-40-8 p-1-ph * n * ⁿ Bu F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-41-1 CH ₃ N n n Bz F F H OH H H XV-41-2 CH ₃ N n CH ₃ Bz F F H OH H H XV-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz F F H OH H H XV-41-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-41-5 CH ₃ n n CH ₂ Ph Bz F F H OH H H XV-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz F F H OH H H XV-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-41-8 CH ₃ * n * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-42-1 Et H H H Bz F F H OH H H XV-42-2 Et H H CH ₃ Bz F F H OH H H XV-42-3 Et H H CH (CH ₃ ) ₂ Bz F F H OH H H XV-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-42-5 Et H H CH ₂ Ph Bz F F H OH H H XV-42-6 Et H H CH ₂ -indol-3-yl Bz F F H OH H H XV-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-42-8 Et * H * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-43-1 ⁱ Pr N n n Bz F F H OH H H XV-43-2 ⁱ Pr N n CH ₃ Bz F F H OH H H XV-43-3 ⁱ Pr N n CH (CH ₃ ) ₂ Bz F F H OH H H XV-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-43-5 ⁱ Pr n n CH ₂ Ph Bz F F H OH H H XV-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz F F H OH H H XV-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-43-8 ⁱ Pr * n * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-44-1 ^t Bu N N n Bz F F H OH H H XV-44-2 ^t Bu N n CH ₃ Bz F F H OH H H XV-44-3 ^t Bu N n CH (CH ₃ ) ₂ Bz F F H OH H H XV-44-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-44-5 ^t Bu N n CH ₂ Ph Bz F F H OH H H XV-44-6 ^t Bu N n CH ₂ -indol-3-yl Bz F F H OH H H XV-44-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-44-8 ^t Bu * n * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-45-1 Ph H H H Bz F F H OH H H XV-45-2 Ph H H CH ₃ Bz F F H OH H H XV-45-3 Ph H H CH (CH ₃ ) ₂ Bz F F H OH H H XV-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-45-5 Ph H H CH ₂ Ph Bz F F H OH H H XV-45-6 Ph H H CH ₂ -indol-3-yl Bz F F H OH H H XV-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-45-8 Ph * H * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-46-1 p-me-ph H H H Bz F F H OH H H XV-46-2 p-me-ph H H CH ₃ Bz F F H OH H H XV-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz F F H OH H H XV-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-46-5 p-me-ph H H CH ₂ Ph Bz F F H OH H H XV-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz F F H OH H H XV-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-46-8 p-me-ph * H * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-47-1 p-f-ph H H H Bz F F H OH H H XV-47-2 p-f-ph H H CH ₃ Bz F F H OH H H XV-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz F F H OH H H XV-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-47-5 p-f-ph H H CH ₂ Ph Bz F F H OH H H XV-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz F F H OH H H XV-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-47-8 p-f-ph * H * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-48-1 p-Cl-Ph H H H Bz F F H OH H H XV-48-2 p-Cl-Ph H H CH ₃ Bz F F H OH H H XV-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz F F H OH H H XV-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-48-5 p-Cl-Ph H H CH ₂ Ph Bz F F H OH H H XV-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz F F H OH H H XV-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-48-8 p-Cl-Ph * H * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XV-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-49-1 p-Br-Ph H H H Bz F F H OH H H XV-49-2 p-Br-Ph H H CH ₃ Bz F F H OH H H XV-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz F F H OH H H XV-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-49-5 p-Br-Ph H H CH ₂ Ph Bz F F H OH H H XV-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz F F H OH H H XV-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-49-8 p-Br-Ph * H * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XV-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XV-50-1 p-1-ph N N n Bz F F H OH H H XV-50-2 p-1-ph N N CH ₃ Bz F F H OH H H XV-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz F F H OH H H XV-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz F F H OH H H XV-50-5 p-1-ph N n CH ₂ Ph Bz F F H OH H H XV-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz F F H OH H H XV-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz F F H OH H H XV-50-8 p-1-ph * n * Bz F F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-1-1 CH ₃ N N n CH ₃ F F F IT N N XVI-1-2 CH ₃ N N CH ₃ CH ₃ F F F IT N N XVI-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ F F F IT N N XVI-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT N N XVI-1-5 CH ₃ N n CH ₂ Ph CH ₃ F F F IT N n XVI-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ F F F IT N n XVI-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n n Xvi-1-8 CH ₃ * n * CH ₃ F F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xvi-2-1 Et H H H CH ₃ F F F IT n n Xvi-2-2 Et H H CH ₃ CH ₃ F F F IT n n XVI-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ F F F IT n n Xvi-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT n n Xvi-2-5 Et H H CH ₂ Ph CH ₃ F F F IT n n Xvi-2-6 Et H H CH ₂ -indol-3-yl CH ₃ F F F IT n n Xvi-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n n Xvi-2-8 Et * H * CH ₃ F F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xvi-3-1 ⁱ Pr N N N CH ₃ F F F IT N N XVI-3-2 ⁱ Pr N N CH ₃ CH ₃ F F F IT N N Xvi-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ F F F IT N N Xvi-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT N N XVI-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ F F F IT N N Xvi-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ F F F IT n N Xvi-3-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n N Xvi-3-8 ⁱ Pr * N * CH ₃ F F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xvi-4-1 ^t Bu N N N CH ₃ F F F IT n n XVI-4-2 ^t Bu N N CH ₃ CH ₃ F F F IT n n Xvi-4-3 ^t Bu N N CH (CH ₃ ) ₂ CH ₃ F F F it n n Xvi-4-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F it n n Xvi-4-5 ^t Bu N N Chzph CH ₃ F F F it n n Xvi-4-6 ^t Bu N N CH ₂ -indol-3-yl CH ₃ F F F it n n Xvi-4-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ CH ₃ F F F it n n Xvi-4-8 ^t Bu * N * CH ₃ F F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-5-1 Ph H H H CH ₃ F F F IT N n Xvi-5-2 Ph H H CH ₃ CH ₃ F F F IT N n XVI-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-5-5 Ph H H CH ₂ Ph CH ₃ F F F IT n n Xvi-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ F F F IT n n Xvi-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n n Xvi-5-8 Ph * H * CH ₃ F F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xvi-6-1 p-me-ph H H H CH ₃ F F F IT N N Xvi-6-2 p-me-ph H H CH ₃ CH ₃ F F F IT N N XVI-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ F F F IT N N Xvi-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT N N Xvi-6-5 p-me-ph H H CH ₂ Ph CH ₃ F F F IT N N Xvi-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ F F F IT N N Xvi-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT N N Xvi-6-8 p-me-ph * H * CH ₃ F F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xvi-7-1 p-f-ph H H H CH ₃ F F F IT N n Xvi-7-2 p-f-ph H H CH ₃ CH ₃ F F F IT n n XVI-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT n n Xvi-7-6 p-f-ph H H CH ₂ Ph CH ₃ F F F IT n n Xvi-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ F F F IT n n Xvi-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n n Xvi-7-20 p-f-ph * H * CH ₃ F F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-8-1 p-Cl-Ph H H H CH ₃ F F F IT N N XVI-8-2 p-Cl-Ph H H CH ₃ CH ₃ F F F IT N N XVI-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ F F F IT N N Xvi-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT N N Xvi-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ F F F IT N N Xvi-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ F F F IT N n Xvi-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT N n Xvi-8-8 p-Cl-Ph * H * CH ₃ F F F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-9-1 p-Br-Ph H H H CH ₃ F F F IT N n XVI-9-2 p-Br-Ph H H CH ₃ CH ₃ F F F IT N n XVI-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ F F F IT n n Xvi-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ F F F IT n n Xvi-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n n XVI-9-20 p-Br-Ph * H * CH ₃ F F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-10-1 p-1-ph n N n CH ₃ F F F IT N n XVI-10-2 p-1-ph n N CH ₃ CH ₃ F F F IT N n XVI-10-3 p-1-ph n N CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-10-4 p-1-ph n N CH ₂ CH (CH ₃ ) ₂ CH ₃ F F F IT n n XVI-10-5 p-1-ph n N CH ₂ Ph CH ₃ F F F IT n n XVI-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ F F F IT n n Xvi-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ F F F IT n n Xvi-10-8 p-1-ph * n * CH ₃ F F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-11-1 CH ₃ N n n Et F F F OH H H XVI-11-2 CH ₃ N n CH ₃ Et F F F OH H H XVI-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et F F F OH H H XVI-11-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-11-5 CH ₃ n n CH ₂ Ph Et F F F OH H H XVI-11-6 CH ₃ n n CH ₂ -indol-3-yl Et F F F OH H H XVI-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et F F F OH H H Xvi-11-8 CH ₃ * n * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-12-1 Et H H H Et F F F OH H H XVI-12-2 Et H H CH ₃ Et F F F OH H H XVI-12-3 Et H H CH (CH ₃ ) ₂ Et F F F OH H H XVI-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-12-5 Et H H CH ₂ Ph Et F F F OH H H XVI-12-6 Et H H CH ₂ -indol-3-yl Et F F F OH H H Xvi-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et F F F OH H H Xvi-12-8 Et * H * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-13-1 ⁱ Pr N n n Et F F F OH H H XVI-13-2 ⁱ Pr N n CH ₃ Et F F F OH H H XVI-13-3 ⁱ Pr n n CH (CH ₃ ) ₂ Et F F F OH H H XVI-13-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-13-5 ⁱ Pr n n CH ₂ Ph Et F F F OH H H XVI-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et F F F OH H H XVI-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-13-8 ⁱ Pr * n * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-14-1 ^t Bu N n n Et F F F OH H H XVI-14-2 ^t Bu N n CH ₃ Et F F F OH H H XVI-14-3 ^t Bu N n CH (CH ₃ ) ₂ Et F F F OH H H XVI-14-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-14-5 ^t Bu N n CH ₂ Ph Et F F F OH H H XVI-14-6 ^t Bu N n CH ₂ -indol-3-yl Et F F F OH H H XVI-14-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-14-8 ^t Bu * n * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-15-1 Ph H H H Et F F F OH H H XVI-15-2 Ph H H CH ₃ Et F F F OH H H XVI-15-3 Ph H H CH (CH ₃ ) ₂ Et F F F OH H H XVI-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-15-5 Ph H H CH ₂ Ph Et F F F OH H H XVI-15-6 Ph H H CH ₂ -indol-3-yl Et F F F OH H H XVI-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-15-8 Ph * H * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-16-1 p-me-ph H H H Et F F F OH H H XVI-16-2 p-me-ph H H CH ₃ Et F F F OH H H XVI-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et F F F OH H H XVI-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-16-5 p-me-ph H H CH ₂ Ph Et F F F OH H H XVI-16-6 p-me-ph H H CH ₂ -indol-3-yl Et F F F OH H H XVI-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-16-8 p-me-ph * H * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-17-1 p-f-ph H H H Et F F F OH H H XVI-17-2 p-f-ph H H CH ₃ Et F F F OH H H XVI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et F F F OH H H XVI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-17-5 p-f-ph H H CH ₂ Ph Et F F F OH H H XVI-17-6 p-f-ph H H CH ₂ -indol-3-yl Et F F F OH H H XVI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-17-8 p-f-ph * H * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-18-1 p-Cl-Ph H H H Et F F F OH H H XM-18-2 p-Cl-Ph H H CH ₃ Et F F F OH H H XVI-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et F F F OH H H XVI-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-18-5 p-Cl-Ph H H CH ₂ Ph Et F F F OH H H XVI-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et F F F OH H H XVI-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-18-8 p-Cl-Ph * H Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-19-1 p-Br-Ph H H H Et F F F OH H H XVI-19-2 p-Br-Ph H H CH ₃ Et F F F OH H H XVI-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et F F F OH H H XVI-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et F F F OH H H XVI-19-5 p-Br-Ph H H CH ₂ Ph Et F F F OH H H XVI-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et F F F OH H H XVI-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et F F F OH H H XVI-19-8 p-Br-Ph * H * Et F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ XVI-20-1 p-1-ph N N N Et F F F OH H XVI-20-2 p-1-ph N N CH ₃ Et F F F OH H XVI-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et F F F OH H XVI-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et F F F OH H XVI-20-5 p-1-ph N N CH ₂ Ph Et F F F OH H XVI-20-6 p-1-ph N N CH ₂ -indol-3-yl Et F F F OH H XVI-20-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Et F F F OH H XVI-20-8 p-1-ph * N * Et F F F OH H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-21-1 CH ₃ N N n ⁱ Pr F F F IT n n XVI-21-2 CH ₃ N N CH ₃ ⁱ Pr F F F IT n n XVI-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr F F F IT n n XVI-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F it n n XVI-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr F F F it n n XVI-21-6 CH ₃ N N CH ₂ -indol-3-yl ⁱ Pr F F F it n n XVI-21-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F it n n XVI-21-8 CH ₃ * N * ⁱ Pr F F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-22-1 Et H H H ⁱ Pr F F F OH H H XVI-22-2 Et H H CH ₃ ⁱ Pr F F F OH H H XVI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-22-5 Et H H CH ₂ Ph ⁱ Pr F F F OH H H XVI-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr F F F OH H H XVI-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F OH H H XVI-22-8 Et * H * ⁱ Pr F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-23-1 ⁱ Pr N N n ⁱ Pr F F F IT N N XVI-23-2 ⁱ Pr N N CH ₃ ⁱ Pr F F F IT N N XVI-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr F F F IT N N XVI-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F IT N N XVI-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr F F F IT N N XVI-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁱ Pr F F F IT N N XVI-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F IT N N XVI-23-8 ⁱ Pr * N * ⁱ Pr F F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-24-1 ^t Bu N n n ⁱ Pr F F F IT N n XVI-24-2 ^t Bu N n CH ₃ ⁱ Pr F F F IT N n XVI-24-3 ^t Bu N n CH (CH ₃ ) ₂ ⁱ Pr F F F IT N n XV1-24-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F IT N n XVI-24-5 ^t Bu N n CH ₂ Ph ⁱ Pr F F F IT N n XVI-24-6 ^t Bu N n CH ₂ -indol-3-yl ⁱ Pr F F F IT N n XVI-24-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F IT N n XVI-24-8 ^t Bu * n * ⁱ Pr F F F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-25-1 Ph H H H ⁱ Pr F F F OH H H XVI-25-2 Ph H H CH ₃ ⁱ Pr F F F OH H H XVI-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-25-5 Ph H H CH ₂ Ph ⁱ Pr F F F OH H H XVI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr F F F OH H H XVI-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F OH H H XVI-25-8 Ph * H * ⁱ Pr F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-26-1 p-me-ph H H H ⁱ Pr F F F OH H H XVI-26-2 p-me-ph H H CH ₃ ⁱ Pr F F F OH H H XVI-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr F F F OH H H XVI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr F F F OH H H XVI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F OH H H XVI-26-8 p-me-ph * H * ⁱ Pr F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-27-1 p-f-ph H H H ⁱ Pr F F F OH H H XVI-27-2 p-f-ph H H CH ₃ ⁱ Pr F F F OH H H XVI-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr F F F OH H H XVI-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr F F F OH H H XVI-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F OH H H XVI-27-8 p-f-ph * H * ⁱ Pr F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVT-28-1 p-Cl-Ph H H H ⁱ Pr F F F OH H H XVI-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr F F F OH H H XVI-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr F F F OH H H XVI-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr F F F OH H H XVI-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F OH H H XVI-28-8 p-Cl-Ph * H * ⁱ Pr F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-29-1 p-Br-Ph H H H ⁱ Pr F F F OH H H XVI-29-2 p-Br-Ph H H CH ₃ ⁱ Pr F F F OH H H XVI-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F OH H H XVI-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr F F F OH H H XVI-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr F F F OH H H XVI-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F OH H H XVI-29-8 p-Br-Ph * H * ⁱ Pr F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-30-1 p-1-ph N n n ⁱ Pr F F F IT N N XVI-30-2 p-1-ph N n CH ₃ ⁱ Pr F F F IT N N XVI-30-3 p-1-ph N n CH (CH ₃ ) ₂ ⁱ Pr F F F IT N N XVI-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr F F F IT N N XVI-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr F F F IT N N XVI-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr F F F IT N N XVI-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr F F F IT N N XVI-30-8 p-1-ph * n * ⁱ Pr F F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-31-1 CH ₃ N N N ⁿ Bu F F F OH H H XVI-31-2 CH ₃ N N CH ₃ ⁿ Bu F F F OH H H XVI-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu F F F OH H H XVI-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-31-8 CH ₃ * N * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-32-1 Et H H H ⁿ Bu F F F OH H H XVI-32-2 Et H H CH ₃ ⁿ Bu F F F OH H H XVI-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-32-5 Et H H CH ₂ Ph ⁿ Bu F F F OH H H XVI-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-32-8 Et * H * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-33-1 ⁱ Pr N n N ⁿ Bu F F F OH H H XVI-33-2 ⁱ Pr n n CH ₃ ⁿ Bu F F F OH H H XVI-33-3 ⁱ Pr n n CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-33-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-33-5 ⁱ Pr n n CISR ⁿ Bu F F F OH H H XVI-33-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-33-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-33-8 ⁱ Pr * n * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-34-1 ^t Bu N n n ⁿ Bu F F F IT N n XVI-34-2 ^t Bu N n CH ₃ ⁿ Bu F F F IT N n XVI-34-3 ^t Bu N n CH (CH ₃ ) ₂ ⁿ Bu F F F IT n n XVI-34-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F IT n n XVI-34-5 ^t Bu N n CH ₂ Ph ⁿ Bu F F F IT n n XVI-34-6 ^t Bu N n CH ₂ -indol-3-yl ⁿ Bu F F F IT n n XVI-34-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F IT n n XVI-34-8 ^t Bu * n * ⁿ Bu F F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-35-1 Ph H H H ⁿ Bu F F F OH H H XVI-35-2 Ph H H CH ₃ ⁿ Bu F F F OH H H XVI-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-35-5 Ph H H CH ₂ Ph ⁿ Bu F F F OH H H XVI-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-35-8 Ph * H * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-36-1 p-me-ph H H H ⁿ Bu F F F OH H H XVI-36-2 p-me-ph H H CH ₃ ⁿ Bu F F F OH H H XVI-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu F F F OH H H XVI-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-36-8 p-me-ph * H * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-37-1 p-f-ph H H H ⁿ Bu F F F OH H H XVI-37-2 p-f-ph H H CH ₃ ⁿ Bu F F F OH H H XVI-37.3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu F F F OH H H XVI-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-37-8 p-f-ph * H * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-38-1 p-Cl-Ph H H H ⁿ Bu F F F OH H H XVI-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu F F F OH H H XVI-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu F F F OH H H XVI-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-38-8 p-Cl-Ph * H * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-39-1 p-Br-Ph H H H ⁿ Bu F F F OH H H XVI-39-2 p-Br-Ph H H CH ₃ ⁿ Bu F F F OH H H XVI-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu F F F OH H H XVI-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-39-8 p-Br-Ph * H * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-40-1 p-1-ph N N n ⁿ Bu F F F OH H H XVI-40-2 p-1-ph N N CH ₃ ⁿ Bu F F F OH H H XVI-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu F F F OH H H XVI-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu F F F OH H H XVI-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu F F F OH H H XVI-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu F F F OH H H XVI-40-8 p-1-ph * n * ⁿ Bu F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-41-1 CH ₃ N N N Bz F F F OH H H XVI-41-2 CH ₃ N n CH ₃ Bz F F F OH H H XVI-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz F F F OH H H XVI-41-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVI-41-5 CH ₃ N N CH ₂ Ph Bz F F F OH H H XVI-41-6 CH ₃ N N CH ₂ -indol-3-yl Bz F F F OH H H XVI-41-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVI-41-8 CH ₃ * N * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-42-1 Et H H H Bz F F F OH H H XVI-42-2 Et H H CH ₃ Bz F F F OH H H XVI-42-3 Et H H CH (CH ₃ ) ₂ Bz F F F OH H H XVI-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVI-42-5 Et H H CH ₂ Ph Bz F F F OH H H XVI-42-6 Et H H CH ₂ -indol-3-yl Bz F F F OH H H XVI-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz F F F OH H H Xvi-42-8 Et * H * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-43-1 ⁱ Pr N n n Bz F F F OH H H XVI-43-2 ⁱ Pr N n CH ₃ Bz F F F OH H H XVI-43-3 ⁱ Pr N n CH (CH ₃ ) ₂ Bz F F F OH H H XVI-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVI-43-5 ⁱ Pr N n CH ₂ Ph Bz F F F OH H H XVI-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz F F F OH H H XVI-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVI-43-8 ⁱ Pr * n * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVI-44-1 ^t Bu N n n Bz F F F OH H H XVI-44-2 ^t Bu N n CH ₃ Bz F F F OH H H XVI-44-3 ^t Bu N n CH (CH ₃ ) ₂ Bz F F F OH H H XVI-44-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVI-44-5 ^t Bu N n CH ₂ Ph Bz F F F OH H H XVI-44-6 ^t Bu N n CH ₂ -indol-3-yl Bz F F F OH H H XVI-44-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVI-44-8 ^t Bu * n * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVH-45-1 Ph H H H Bz F F F OH H H XVn-45-2 Ph H H CH ₃ Bz F F F OH H H XVII-45-3 Ph H H CH (CH ₃ ) ₂ Bz F F F OH H H XVII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVII-45-5 Ph H H CH ₂ Ph Bz F F F OH H H XVII-45-6 Ph H H CH ₂ -indol-3-yl Bz F F F OH H H XVII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVII-45-8 Ph * H * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVII-46-1 p-me-ph H H H Bz F F F OH H H XVII-46-2 p-me-ph H H CH ₃ Bz F F F OH H H XVII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz F F F OH H H XVII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVII-46-5 p-me-ph H H CH ₂ Ph Bz F F F OH H H XVII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz F F F OH H H XVII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVII-46-8 p-me-ph * H * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVII-47-1 p-f-ph H H H Bz F F F OH H H XVII-47-2 p-f-ph H H CH ₃ Bz F F F OH H H XVII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz F F F OH H H XVII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVII-47-5 p-f-ph H H CH ₂ Ph Bz F F F OH H H XVII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz F F F OH H H XVII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVII-47-8 p-f-ph * H * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVII-48-1 p-Cl-Ph H H H Bz F F F OH H H XVII-48-2 p-Cl-Ph H H CH ₃ Bz F F F OH H H XVII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz F F F OH H H XVII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVII-48-5 p-Cl-Ph H H CH ₂ Ph Bz F F F OH H H XVII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz F F F OH H H XVII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVII-48-8 p-Cl-Ph * H * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVI-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVII-49-1 p-Br-Ph H H H Bz F F F OH H H XVII-49-2 p-Br-Ph H H CH ₃ Bz F F F OH H H XVII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz F F F OH H H XVII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVII-49-5 p-Br-Ph H H CH ₂ Ph Bz F F F OH H H XVII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz F F F OH H H XVII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVII-49-8 p-Br-Ph * H * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVI-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVII-50-1 p-1-ph N n n Bz F F F OH H H XVII-50-2 p-1-ph N n CH ₃ Bz F F F OH H H XVII-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz F F F OH H H XVII-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz F F F OH H H XVII-50-5 p-1-ph n n CH ₂ Ph Bz F F F OH H H XVII-50-6 p-1-ph n n CH ₂ -indol-3-yl Bz F F F OH H H XVII-50-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Bz F F F OH H H XVII-50-8 p-1-ph * n * Bz F F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-1-1 CH ₃ N N n CH ₃ OCH ₃ F n IT n n XVIII-1-2 CH ₃ N N CH ₃ CH ₃ OCH ₃ F n IT n n XVIII-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-1-5 CH ₃ N n CH ₂ Ph CH ₃ OCH ₃ F n it n n XVIII-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ OCH ₃ F n it n n XVIII-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F n it n n XVIII-1-8 CH ₃ * n * CH ₃ OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xviii-2-1 Et H H H CH ₃ Och ₃ F H OH H H XVIII-2-2 Et H H CH ₃ CH ₃ Och ₃ F H OH H H XVIII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ Och ₃ F H OH H H Xviii-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ Och ₃ F H OH H H Xviii-2-5 Et H H CH ₂ Ph CH ₃ Och ₃ F H OH H H XVIII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ Och ₃ F H OH H H Xviii-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ Och ₃ F H OH H H Xviii-2-8 Et * H * CH ₃ Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-3-1 ⁱ Pr N n n CH ₃ OCH ₃ F N it n n XVIII-3-2 ⁱ Pr N n sun ₃ CH ₃ OCH ₃ F n it n n XVIII-3-3 ⁱ Pr n n CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-3-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-3-5 ⁱ Pr n n CH ₂ Ph CH ₃ OCH ₃ F n it n n XVIII-3-6 ⁱ Pr n n CH ₂ -indol-3-yl CH ₃ OCH ₃ F n it n n XVIII-3-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F n it n n XVIII-3-8 ⁱ Pr * n * CH ₃ OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-4-1 ^t Bu N n n CH ₃ OCH ₃ F N IT N N XVIII-4-2 ^t Bu N n CH ₃ CH ₃ OCH ₃ F N IT N N XVIII-4-3 ^t Bu N n CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT n n XVIII-4-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT n n Xviii-4-5 ^t Bu N n CH ₂ Ph CH ₃ OCH ₃ F N IT n n XVIII-4-6 ^t Bu N n CH ₂ -indol-3-yl CH ₃ OCH ₃ F N IT n n XVIII-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F N IT n n XVIII-4-8 ^t Bu * n * CH ₃ OCH ₃ F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-5-1 Ph H H H CH ₃ OCH ₃ F N IT n n XVIII-5-2 Ph H H CH ₃ CH ₃ OCH ₃ F N IT n n XVIII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n IT n n XVIII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-5-5 Ph H H CH ₂ Ph CH ₃ OCH ₃ F n it n n XVIII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F n it n n Xviii-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F n it n n Xviii-5-8 Ph * H * CH ₃ OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-6-1 p-me-ph H H H CH ₃ OCH ₃ F N IT N N Xviii-6-2 p-me-ph H H CH ₃ CH ₃ OCH ₃ F N IT N N Xviii-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT N N Xviii-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT N N XVIII-6-5 p-me-ph H H CH ₂ Ph CH ₃ OCH ₃ F N IT N N XVIII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F N IT N N XVIII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F N IT n N XVIII-6-8 p-me-ph H * CH ₃ OCH ₃ F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-7-1 p-f-ph H H H CH ₃ OCH ₃ F N IT N n XVIII-7-2 p-f-ph H H CH ₃ CH ₃ OCH ₃ F N IT N n Xviii-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT N n XVIII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT N n Xviii-7-6 p-f-ph H H CH ₂ Ph CH ₃ OCH ₃ F N IT N n XVIII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F N IT N n XVIII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F N IT N n Xviii-7-20 p-f-ph * H * CH ₃ OCH ₃ F N IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-8-1 p-Cl-Ph H H H CH ₃ OCH ₃ F N IT N n XVIII-8-2 p-Cl-Ph H H CH ₃ CH ₃ OCH ₃ F N IT N n XVIII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT N n Xviii-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F N IT n n XVIII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ OCH ₃ F N IT n n Xviii-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F N IT n n XVIII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F N IT n n XVIII-8-8 p-Cl-Ph * H * CH ₃ OCH ₃ F N it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-9-1 p-Br-Ph H H H CH ₃ OCH ₃ F N IT n n XVIII-9-2 p-Br-Ph H H CH ₃ CH ₃ OCH ₃ F n IT n n XVIII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ OCH ₃ F n it n n Xviii-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F n it n n XVIII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F n it n n XVHI-9-20 p-Br-Ph * H * CH ₃ OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xviii-10-1 p-1-ph N N n CH ₃ OCH ₃ F n IT n n Xviii-10-2 p-1-ph N N CH ₃ CH ₃ OCH ₃ F n IT n n XVIII-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F n it n n XVIII-10-5 p-1-ph N n CH ₂ Ph CH ₃ OCH ₃ F n it n n XV1II-10-6 p-1-ph N N CH ₂ -indol-3-yl CH ₃ OCH ₃ F n it n n XVIII-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F n it n n XVIII-10-8 p-1-ph * N * CH ₃ OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-11-1 CH ₃ N n n Et OCH ₃ F H OH H H XVIII-11-2 CH ₃ N n CH ₃ Et Och ₃ F H OH H H XVIII-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-11-5 CH ₃ N n CH ₂ Ph Et Och ₃ F H OH H H XVIII-11-6 CH ₃ N n CH ₂ -indol-3-yl Et Och ₃ F H OH H H XVIII-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et Och ₃ F H OH H H XVIII-11-8 CH ₃ * n * Et Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-12-1 Et H H H Et Och ₃ F H OH H H XVIII-12-2 Et H H CH ₃ Et Och ₃ F H OH H H XVIII-12-3 Et H H CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-12-5 Et H H CH ₂ Ph Et Och ₃ F H OH H H XVIII-12-6 Et H H CH ₂ -indol-3-yl Et Och ₃ F H OH H H XVIII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F H OH H H XVIII-12-8 Et * H * Et Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-13-1 ⁱ Pr N n n Et Och ₃ F H OH H H XVIII-13-2 ⁱ Pr N n CH ₃ Et Och ₃ F H OH H H XVIII-13-3 ⁱ Pr n n CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-13-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-13-5 ⁱ Pr n n CH ₂ Ph Et Och ₃ F H OH H H XVIII-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et Och ₃ F H OH H H XVIII-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et Och ₃ F H OH H H XVIII-13-8 ⁱ Pr * n * Et Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-14-1 ^t Bu n N n Et Och ₃ F H OH H H XVIII-14-2 ^t Bu n N CH ₃ Et Och ₃ F H OH H H XVIII-14-3 ^t Bu n N CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-14-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-14-5 ^t Bu n n CH ₂ Ph Et Och ₃ F H OH H H XVIII-14-6 ^t Bu n n CH ₂ -indol-3-yl Et Och ₃ F H OH H H Xviii-14-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Et Och ₃ F H OH H H XVIII-14-8 ^t Bu * n * Et Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-15-1 Ph H H H Et Och ₃ F H OH H H XVIII-15-2 Ph H H CH ₃ Et Och ₃ F H OH H H XVIII-15-3 Ph H H CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-15-5 Ph H H CH ₂ Ph Et Och ₃ F H OH H H XVIII-15-6 Ph H H CH ₂ -indol-3-yl Et Och ₃ F H OH H H XVIII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et OCH ₃ F H OH H H XVIII-15-8 Ph * H * Et OCH ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-16-1 p-me-ph H H H Et Och ₃ F H OH H H XVIII-16-2 p-me-ph H H CH ₃ Et Och ₃ F H OH H H XVIII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-16-5 p-me-ph H H CH ₂ Ph Et Och ₃ F H OH H H XVIII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et Och ₃ F H OH H H XVIII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F H OH H H XVIII-16-8 p-me-ph * H * Et Och ₃ F H OH H H

* R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-17-1 p-f-ph H H H Et OCH ₃ F N IT n n XVIII-17-2 p-f-ph H H CH ₃ Et Och ₃ F n IT n n XVIII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et OCH ₃ F n it n n XVIII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et OCH ₃ F n it n n XVIII-17-5 p-f-ph H H CH ₂ Ph Et OCH ₃ F n it n n XVIII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et OCH ₃ F n it n n XVIII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et OCH ₃ F n it n n XVIII-17-8 p-f-ph * H * Et OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-18-1 p-Cl-Ph H H H Et OCH ₃ F N IT n n XVIII-18-2 p-Cl-Ph H H CH ₃ Et Och ₃ F N IT n n XVIII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et OCH ₃ F n it n n XVIII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et OCH ₃ F n it n n XVIII-18-5 p-Cl-Ph H H CH ₂ Ph Et OCH ₃ F n it n n XVIII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et OCH ₃ F n it n n XVIII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et OCH ₃ F n it n n XVIII-18-8 p-Cl-Ph * H * Et OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-19-1 p-Br-Ph H H H Et OCH ₃ F n IT n n XVIII-19-2 p-Br-Ph H H CH ₃ Et OCH ₃ F n it n n XVIII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et OCH ₃ F n it n n XVIII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et OCH ₃ F n it n n XVIII-19-5 p-Br-Ph H H CH ₂ Ph Et OCH ₃ F n it n n XVIII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et OCH ₃ F n it n n XVIII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et OCH ₃ F n it n n XVIII-19-8 p-Br-Ph * H * Et OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-20-1 p-1-ph N N n Et Och ₃ F H OH H H XVIII-20-2 p-1-ph N N CH ₃ Et Och ₃ F H OH H H XVIII-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F H OH H H XVIII-20-5 p-1-ph N N CH ₂ Ph Et Och ₃ F H OH H H XVIII-20-6 p-1-ph N N CH ₂ -indol-3-yl Et Och ₃ F H OH H H XVIII-20-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Et Och ₃ F H OH H H XVIII-20-8 p-1-ph * N * Et Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-21-1 CH ₃ N N N ⁱ Pr OCH ₃ F N it n n XVIII-21-2 CH ₃ N N CH ₃ ⁱ Pr OCH ₃ F N IT n n XVIII-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F N IT n n XVIII-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n IT n n XVIII-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr OCH ₃ F n IT n n XVIII-21-6 CH ₃ N N CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F n IT n n XVIII-21-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F n IT n n XVIII-21-8 CH ₃ * N * ⁱ Pr OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-22-1 Et H H H ⁱ Pr Och ₃ F H OH H H XVIII-22-2 Et H H CH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-22-5 Et H H CH ₂ Ph ⁱ Pr Och ₃ F H OH H H XVIII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F H OH H H XVIII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-22-8 Et * H * ⁱ Pr Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-23-1 ⁱ Pr n N n ⁱ Pr OCH ₃ F n IT n n XVIII-23-2 ⁱ Pr n N CH ₃ ⁱ Pr OCH ₃ F n it n n XV1II-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n it n n XVIII-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n it n n XVIII-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr OCH ₃ F n it n n XVIII-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F n it n n XVIII-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F n it n n XVIII-23-8 ⁱ Pr * n * ⁱ Pr OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-24-1 ^t Bu n N n ⁱ Pr OCH ₃ F n IT n n XVIII-24-2 ^t Bu N n CH ₃ ⁱ Pr OCH ₃ F n IT n n XVIII-24-Z ^t Bu n n CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n IT n n XVIII-24-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n it n n XVIII-24-5 ^t Bu n n CH ₂ Ph ⁱ Pr OCH ₃ F n it n n XVIII-24-6 ^t Bu N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F n it n n XVIII-24-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F n it n n XVIII-24-8 ^t Bu * n * ⁱ Pr OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-25-1 Ph H H H ⁱ Pr Och ₃ F H OH H H XVIII-25-2 Ph H H CH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-25-5 Ph H H CH ₂ Ph ⁱ Pr Och ₃ F H OH H H XVIII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F H OH H H XVIII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-25-8 Ph * H * ⁱ Pr Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-26-1 p-me-ph H H H ⁱ Pr OCH ₃ F N IT n n XVIII-26-2 p-me-ph H H CH ₃ ⁱ Pr Och ₃ F n IT n n XVIII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n it n n XVIII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F n it n n XVIII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr Och ₃ F n it n n XVIII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F n it n n XVIII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F n it n n XVIII-26-8 p-me-ph * H * ⁱ Pr OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-27-1 p-f-ph H H H ⁱ Pr Och ₃ F H OH H H XVIII-27-2 p-f-ph H H CH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr Och ₃ F H OH H H XVIII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F H OH H H Xviii-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-27-8 p-f-ph * H * ⁱ Pr Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-28-1 p-Cl-Ph H H H ⁱ Pr Och ₃ F H OH H H XVIII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr Och ₃ F H OH H H XVIII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F H OH H H XVIII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-28-8 p-Cl-Ph * H * ⁱ Pr Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-29-1 p-Br-Ph H H H ⁱ Pr Och ₃ F H OH H H XVIII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr Och ₃ F H OH H H XVIII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F H OH H H XVIII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr Och ₃ F H OH H H XVIII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F H OH H H Xviii-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F H OH H H Xviii-29-8 p-Br-Ph * H * ⁱ Pr OCH ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-30-1 p-1-ph N n n ⁱ Pr OCH ₃ F N IT N N XVIII-30-2 p-1-ph N n CH ₃ ⁱ Pr OCH ₃ F N IT N N XVIII-30-3 p-1-ph n n CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F N IT N N XVIII-30-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F N IT N N XVIII-30-5 p-1-ph n n CH ₂ Ph ⁱ Pr OCH ₃ F N IT N N XVIII-30-6 p-1-ph n n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F N IT N N XVIII-30-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F N IT N N XVIII-30-8 p-1-ph * n * ⁱ Pr OCH ₃ F N IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-31-1 CH ₃ N N n ⁿ Bu Och ₃ F H OH H H XVIII-31-2 CH ₃ N N CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-31-6 CH ₃ N N CHg-indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-31-8 CH ₃ * N * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-32-1 Et H H H ⁿ Bu OCH ₃ F n IT n n XVIII-32-2 Et H H CH ₃ ⁿ Bu Och ₃ F n IT n n XVIII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu OCH ₃ F n IT n n XVIII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu OCH ₃ F n it n n XVIII-32-5 Et H H CH ₂ Ph ⁿ Bu OCH ₃ F n it n n XVIII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu OCH ₃ F n it n n XVIII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu OCH ₃ F n it n n XVIII-32-8 Et * H * ⁿ Bu OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-33-1 ⁱ Pr n n n ⁿ Bu Och ₃ F H OH H H XVI1I-33-2 ⁱ Pr n N CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-33-4 ⁱ Pr n N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-33-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-33-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-33-8 ⁱ Pr * n * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-34-1 ^t Bu N N n ⁿ Bu OCH ₃ F N it n n XVIII-34-2 ^t Bu N N CH ₃ ⁿ Bu OCH ₃ F N IT n n XVIII-34-3 ^t Bu N N CH (CH ₃ ) ₂ ⁿ Bu OCH ₃ F n IT n n XVIII-34-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu OCH ₃ F n it n n XVIII-34-5 ^t Bu N n CH ₂ Ph ⁿ Bu OCH ₃ F n it n n XVIII-34-6 ^t Bu N n CH ₂ -indol-3-yl ⁿ Bu OCH ₃ F n it n n Xviii-34-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu OCH ₃ F n it n n XVIII-34-8 ^t Bu * n * ⁿ Bu OCH ₃ F n it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-35-1 Ph H H H ⁿ Bu Och ₃ F H OH H H XVIII-35-2 Ph H H CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-35-5 Ph H H CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-35-8 Ph * H * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-36-1 p-me-ph H H H ⁿ Bu Och ₃ F H OH H H XVIII-36-2 p-me-ph H H CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-36-8 p-me-ph * H * "Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-37-1 p-f-ph H H H ⁿ Bu Och ₃ F H OH H H XVIII-37-2 p-f-ph H H CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-37-8 p-f-ph * H * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-38-1 p-Cl-Ph H H H ⁿ Bu Och ₃ F H OH H H XVIII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-38-8 p-Cl-Ph * H * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-39-1 p-Br-Ph H H H ⁿ Bu Och ₃ F H OH H H XVIII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-39-8 p-Br-Ph * H * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-40-1 p-1-ph N n N ⁿ Bu Och ₃ F H OH H H XVIII-40-2 p-1-ph N n CH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F H OH H H XVIII-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu Och ₃ F H OH H H XVIII-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu Och ₃ F H OH H H XVIII-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F H OH H H XVIII-40-8 p-1-ph * n * ⁿ Bu Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-41-1 CH ₃ N N n Bz Och ₃ F H OH H H XVIII-41-2 CH ₃ N N CH ₃ Bz Och ₃ F H OH H H XVIII-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-41-5 CH ₃ N n CH ₂ Ph Bz Och ₃ F H OH H H XVIII-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVIII-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-41-8 CH ₃ * n * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-42-1 Et H H H Bz Och ₃ F H OH H H Xviii-42-2 Et H H CH ₃ Bz Och ₃ F H OH H H XVIII-42-3 Et H H CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-42-5 Et H H CH ₂ Ph Bz Och ₃ F H OH H H XVIII-42-6 Et H H CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVIII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-42-8 Et * H * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ Xviii-43-1 ⁱ Pr N N n Bz Och ₃ F H OH H H XVIII-43-2 ⁱ Pr N N CH ₃ Bz Och ₃ F H OH H H XVIII-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-43-5 ⁱ Pr N n CH ₂ Ph Bz Och ₃ F H OH H H XVIII-43-b ⁱ Pr N n CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVHI-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-43-8 ⁱ Pr * n Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVHI-44-1 ^t Bu N N n Bz Och ₃ F H OH H H XVHI-44-2 ^t Bu N N CH ₃ Bz Och ₃ F H OH H H XVIII-44-3 ^t Bu N N CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-44-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-44-5 ^t Bu N n CH ₂ Ph Bz Och ₃ F H OH H H XVIII-44-6 ^t Bu N n CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVIII-44-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-44-8 ^t Bu * n * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-45-1 Ph H H H Bz Och ₃ F H OH H H XVIII-45-2 Ph H H CH ₃ Bz Och ₃ F H OH H H XVIII-45-3 Ph H H CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-45-5 Ph H H CH ₂ Ph Bz Och ₃ F H OH H H XVIII-45-6 Ph H H CH ₂ -indol-3-yl Bz Och ₃ F H OH H H Xviii-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-45-8 Ph * H * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVHI-46-1 p-me-ph H H H Bz Och ₃ F H OH H H XVIII-46-2 p-me-ph H H CH ₃ Bz Och ₃ F H OH H H XVIII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-46-5 p-me-ph H H CH ₂ Ph Bz Och ₃ F H OH H H XVIII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVIII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-46-8 p-me-ph * H * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-47-1 p-f-ph H H H Bz Och ₃ F H OH H H XVIII-47-2 p-f-ph H H CH ₃ Bz Och ₃ F H OH H H XVIII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-47-5 p-f-ph H H CH ₂ Ph Bz Och ₃ F H OH H H XVIII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVIII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-47-8 p-f-ph * H * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-48-1 p-Cl-Ph H H H Bz Och ₃ F H OH H H XVIII-48-2 p-Cl-Ph H H CH ₃ Bz Och ₃ F H OH H H XVIII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-48-5 p-Cl-Ph H H CH ₂ Ph Bz Och ₃ F H OH H H XVIII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz Och ₃ F H OH H H XVIII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-48-8 p-Cl-Ph * H * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XVIII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVIII-49-1 p-Br-Ph H H H Bz Och ₃ F H OH H H XVIII-49-2 p-Br-Ph H H CH ₃ Bz Och ₃ F H OH H H XVIII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F H OH H H XVIII-49-5 p-Br-Ph H H CH ₂ Ph Bz Och ₃ F H OH H H XVIII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz Och ₃ F H OH H H Xviii-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F H OH H H XVIII-49-8 p-Br-Ph * H * Bz Och ₃ F H OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XVIII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XVTH-50-1 p-1-ph N n n Bz OCH ₃ F N IT n n XVIII-50-2 p-1-ph N n CH ₃ Bz Och ₃ F N IT n n XVIII-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz OCH ₃ F N IT n n XVIII-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz OCH ₃ F N IT n n XVIII-50-5 p-1-ph N n CH ₂ Ph Bz OCH ₃ F N IT n n XVIII-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz OCH ₃ F N IT n n XVIII-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz OCH ₃ F N IT n n XVIII-50-8 p-1-ph * n * Bz OCH ₃ F N IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-1-1 CH ₃ N N N CH ₃ OCH ₃ F F IT N N XIX-1-2 CH ₃ N N CH ₃ CH ₃ OCH ₃ F F IT N N XIX-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-1-5 CH ₃ N n CH ₂ Ph CH ₃ OCH ₃ F F IT N N XIX-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ OCH ₃ F F IT N N XIX-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F IT N N XIX-1-8 CH ₃ * n * CH ₃ OCH ₃ F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-2-1 Et H H H CH ₃ Och ₃ F F IT N N XIX-2-2 Et H H CH ₃ CH ₃ Och ₃ F F IT N N XIX-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-2-5 Et H H CH ₂ Ph CH ₃ OCH ₃ F F IT N N XIX-2-6 Et H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F F IT N N XIX-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F IT N N XIX-2-8 Et * H * CH ₃ OCH ₃ F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-3-1 ⁱ Pr N N n CH ₃ OCH ₃ F F IT N N XIX-3-2 ⁱ Pr N N CH ₃ CH ₃ OCH ₃ F F IT N N XIX-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ OCH ₃ F F IT N N XIX-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ OCH ₃ F F IT N N XIX-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F IT N N XIX-3-8 ⁱ Pr * n * CH ₃ OCH ₃ F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-4-1 ^t Bu N n n CH ₃ OCH ₃ F F IT N N XIX-4-2 ^t Bu N n CH ₃ CH ₃ OCH ₃ F F IT N N XIX-4-3 ^t Bu n n CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT n N XIX-4-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT n N XIX-4-5 ^t Bu n n CH ₂ Ph CH ₃ OCH ₃ F F IT n N XIX-4-6 ^t Bu n n CH ₂ -indol-3-yl CH ₃ OCH ₃ F F IT n n XIX-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F IT n n XIX-4-8 ^t Bu * n * CH ₃ OCH ₃ F F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-5-1 Ph H H H CH ₃ OCH ₃ F F IT n n XIX-5-2 Ph H H CH ₃ CH ₃ OCH ₃ F F IT n n XIX-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT n n XIX-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT n n XIX-5-5 Ph H H CH ₂ Ph CH ₃ OCH ₃ F F it n n XIX-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F F it n n XIX-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F it n n XIX-5-8 Ph H * CH ₃ OCH ₃ F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-6-1 p-me-ph H H H CH ₃ OCH ₃ F F IT n n XIX-6-2 p-me-ph H H CH ₃ CH ₃ OCH ₃ F F IT n n XIX-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F it n n XIX-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F it n n XIX-6-5 p-me-ph H H CH ₂ Ph CH ₃ OCH ₃ F F it n n XIX-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F F it n n XIX-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F it n n XIX-6-8 p-me-ph H * CH ₃ OCH ₃ F F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-7-1 p-f-ph H H H CH ₃ OCH ₃ F F IT N N XIX-7-2 p-f-ph H H CH ₃ CH ₃ OCH ₃ F F IT N N XIX-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N N XIX-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N n XIX-7-6 p-f-ph H H CH ₂ Ph CH ₃ OCH ₃ F F IT N n XIX-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ F F IT N n XIX-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F IT N n XIX-7-20 p-f-ph * H * CH ₃ OCH ₃ F F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-8-1 p-Cl-Ph H H H CH ₃ Och ₃ F F OH H H XIX-8-2 p-Cl-Ph H H CH ₃ CH ₃ Och ₃ F F OH H H XIX-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ Och ₃ F F OH H H XIX-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ Och ₃ F F OH H H XIX-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ Och ₃ F F OH H H XIX-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ Och ₃ F F OH H H XIX-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ Och ₃ F F OH H H XIX-8-8 p-Cl-Ph * H * CH ₃ Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-9-1 p-Br-Ph H H H CH ₃ Och ₃ F F OH H H XIX-9-2 p-Br-Ph H H CH ₃ CH ₃ Och ₃ F F OH H H XIX-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ Och ₃ F F OH H H XIX-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ Och ₃ F F OH H H XIX-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ Och ₃ F F OH H H XIX-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ Och ₃ F F OH H H XIX-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F OH H H XIX-9-20 p-Br-Ph * H * CH ₃ OCH ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-10-1 p-1-ph N N N CH ₃ OCH ₃ F F IT N N XIX-10-2 p-1-ph N n CH ₃ CH ₃ OCH ₃ F F IT N N XIX-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N n XIX-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ F F IT N n XIX-10-5 p-1-ph N n CH ₂ Ph CH ₃ OCH ₃ F F IT N n XIX-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ OCH ₃ F F IT N n XIX-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ F F IT N n XIX-10-8 p-1-ph * n * CH ₃ OCH ₃ F F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-11-1 CH ₃ N n n Et Och ₃ F F OH H H XIX-11-2 CH ₃ N n CH ₃ Et Och ₃ F F OH H H XIX-11-3 CH ₃ n n CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-11-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-11-5 CH ₃ n n CH ₂ Ph Et Och ₃ F F OH H H XIX-11-6 CH ₃ n n CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-11-8 CH ₃ * n * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-12-1 Et H H H Et Och ₃ F F OH H H XIX-12-2 Et H H CH ₃ Et Och ₃ F F OH H H XIX-12-3 Et H H CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-12-5 Et H H CH ₂ Ph Et Och ₃ F F OH H H XIX-12-6 Et H H CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-12-8 Et * H * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-13-1 ⁱ Pr N n n Et Och ₃ F F OH H H XIX-13-2 ⁱ Pr N n CH ₃ Et Och ₃ F F OH H H XIX-13-3 ⁱ Pr N n CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-13-5 ⁱ Pr n n CH ₂ Ph Et Och ₃ F F OH H H XIX-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-13-8 ⁱ Pr * n * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-14-1 ^t Bu N N n Et OCH ₃ F F OH H H XIX-14-2 ^t Bu N N CH ₃ Et Och ₃ F F OH H H XIX-14-3 ^t Bu N N CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-14-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-14-5 ^t Bu N n CH ₂ Ph Et Och ₃ F F OH H H XIX-14-6 ^t Bu N n CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-14-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-14-8 ^t Bu * n * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-15-1 Ph H H H Et Och ₃ F F OH H H XIX-15-2 Ph H H CH ₃ Et Och ₃ F F OH H H XIX-15-3 Ph H H CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-15-5 Ph H H CH ₂ Ph Et Och ₃ F F OH H H XIX-15-6 Ph H H CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-15-8 Ph * H * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-16-1 p-me-ph H H H Et Och ₃ F F OH H H XIX-16-2 p-me-ph H H CH ₃ Et Och ₃ F F OH H H XIX-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-16-5 p-me-ph H H CH ₂ Ph Et Och ₃ F F OH H H XIX-16-6 p-me-ph H H CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-16-8 p-me-ph * H * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-17-1 p-f-ph H H H Et Och ₃ F F OH H H XIX-17-2 p-f-ph H H CH ₃ Et Och ₃ F F OH H H XIX-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-17-5 p-f-ph H H CH ₂ Ph Et Och ₃ F F OH H H XIX-17-6 p-f-ph H H CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-17-8 p-f-ph * H * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-18-1 p-Cl-Ph H H H Et Och ₃ F F OH H H XIX-18-2 p-Cl-Ph H H CH ₃ Et Och ₃ F F OH H H XIX-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-18-5 p-Cl-Ph H H CH ₂ Ph Et Och ₃ F F OH H H XIX-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-18-8 p-Cl-Ph * H * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-19-1 p-Br-Ph H H H Et Och ₃ F F OH H H XIX-19-2 p-Br-Ph H H CH ₃ Et Och ₃ F F OH H H XIX-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H H XIX-19-5 p-Br-Ph H H CH ₂ Ph Et Och ₃ F F OH H H XIX-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et Och ₃ F F OH H H XIX-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H H XIX-19-8 p-Br-Ph * H * Et Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ XIX-20-1 p-1-ph N n n Et Och ₃ F F OH H XIX-20-2 p-1-ph N n CH ₃ Et Och ₃ F F OH H XIX-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et Och ₃ F F OH H XIX-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ F F OH H XIX-20-5 p-1-ph N n CH ₂ Ph Et Och ₃ F F OH H XIX-20-6 p-1-ph N n CH ₂ -indol-3-yl Et Och ₃ F F OH H XIX-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et Och ₃ F F OH H XIX-20-8 p-1-ph * n * Et Och ₃ F F OH H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-21-1 CH ₃ N N n ⁱ Pr OCH ₃ F F IT N N XIX-21-2 CH ₃ N N CH ₃ ⁱ Pr OCH ₃ F F IT N N XIX-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F IT N N XIX-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F IT N N XIX-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr OCH ₃ F F IT N N XIX-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F F IT N N XIX-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F F IT N N XIX-21-8 CH ₃ * n * ⁱ Pr OCH ₃ F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-22-1 Et H H H ⁱ Pr Och ₃ F F OH H H XIX-22-2 Et H H CH ₃ ⁱ Pr Och ₃ F F OH H H XIX-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-22-5 Et H H CH ₂ Ph ⁱ Pr Och ₃ F F OH H H XIX-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F F OH H H XIX-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F F OH H H XIX-22-8 Et * H * ⁱ Pr Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-23-1 ⁱ Pr N N N ⁱ Pr OCH ₃ F F IT N N XIX-23-2 ⁱ Pr N N CH ₃ ⁱ Pr OCH ₃ F F IT N N XIX-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F IT N N XIX-23-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F IT N N XIX-23-5 ⁱ Pr N N CH ₂ Ph ⁱ Pr OCH ₃ F F IT N N XIX-23-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F F IT N N XIX-23-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F F IT N N XIX-23-8 ⁱ Pr * N * ⁱ Pr OCH ₃ F F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-24-1 ⁱ Pr N n n ⁱ Pr OCH ₃ F F IT N N XIX-24-2 ⁱ Pr N n CH ₃ ⁱ Pr OCH ₃ F F IT N N XIX-24-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F IT N N XIX-24-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F IT N N XIX-24-5 ⁱ Pr n n CH ₂ Ph ⁱ Pr OCH ₃ F F IT N N XIX-24-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F F IT N XIX-24-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F F IT N n XIX-24-8 ⁱ Pr * n * ⁱ Pr OCH ₃ F F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-25-1 Ph H H H ⁱ Pr Och ₃ F F OH H H XIX-25-2 Ph H H CH ₃ ⁱ Pr Och ₃ F F OH H H XIX-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-25-5 Ph H H CH ₂ Ph ⁱ Pr Och ₃ F F OH H H XIX-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F F OH H H XIX-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F F OH H H XIX-25-8 Ph * H * ⁱ Pr Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-26-1 p-me-ph H H H ⁱ Pr Och ₃ F F OH H H XIX-26-2 p-me-ph H H CH ₃ ⁱ Pr Och ₃ F F OH H H XIX-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr Och ₃ F F OH H H XIX-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F F OH H H XIX-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F F OH H H XIX-26-8 p-me-ph * H * ⁱ Pr OCH ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-27-1 p-f-ph H H H ⁱ Pr Och ₃ F F OH H H XIX-27-2 p-f-ph H H CH ₃ ⁱ Pr Och ₃ F F OH H H XIX-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr Och ₃ F F OH H H XIX-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F F OH H H XIX-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F F OH H H XIX-27-8 p-f-ph * H * ⁱ Pr Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-28-1 p-Cl-Ph H H H ⁱ Pr Och ₃ F F OH H H XIX-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr Och ₃ F F OH H H XIX-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr Och ₃ F F OH H H XIX-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F F OH H H XIX-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F F OH H H XIX-28-8 p-Cl-Ph * H * ⁱ Pr Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-29-1 p-Br-Ph H H H ⁱ Pr Och ₃ F F OH H H XIX-29-2 p-Br-Ph H H CH ₃ ⁱ Pr Och ₃ F F OH H H XIX-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ F F OH H H XIX-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr Och ₃ F F OH H H XIX-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ F F OH H H XIX-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ F F OH H H XIX-29-8 p-Br-Ph * H * ⁱ Pr Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-30-1 p-1-ph N N n ⁱ Pr OCH ₃ F F OH H H XIX-30-2 p-1-ph N N CH ₃ ⁱ Pr OCH ₃ F F OH H H XIX-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F OH H H XIX-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ F F OH H H XIX-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr OCH ₃ F F OH H H XIX-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ F F OH H H XIX-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ F F OH H H XIX-30-8 p-1-ph * n ⁱ Pr OCH ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-31-1 CH ₃ N N n ⁿ Bu Och ₃ F F OH H H XIX-31-2 CH ₃ N N CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-31-8 CH ₃ * n * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-32-1 Et H H H ⁿ Bu Och ₃ F F OH H H XIX-32-2 Et H H CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-32-5 Et H H CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-32-8 Et * H * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-33-1 ⁱ Pr N N n ⁿ Bu Och ₃ F F OH H H XIX-33-2 ⁱ Pr N n CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-33-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-33-5 ⁱ Pr N n CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-33-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-33-8 ⁱ Pr * n * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-34-1 ^t Bu N n n ⁿ Bu Och ₃ F F OH H H XIX-34-2 ^t Bu N n CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-34-3 ^t Bu N n CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-34-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-34-5 ^t Bu N n CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-34-6 ^t Bu N n CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-34-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-34-8 ^t Bu * n * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-35-1 Ph H H H ⁿ Bu Och ₃ F F OH H H XIX-35-2 Ph H H CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-35-5 Ph H H CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-35-8 Ph * H * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-36-1 p-me-ph H H H ⁿ Bu Och ₃ F F OH H H XIX-36-2 p-me-ph H H CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-36-8 p-me-ph * H ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-37-1 p-f-ph H H H ⁿ Bu Och ₃ F F OH H H XIX-37-2 p-f-ph H H CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-37-8 p-f-ph * H * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-38-1 p-Cl-Ph H H H ⁿ Bu Och ₃ F F OH H H XIX-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-38-8 p-Cl-Ph * H * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-39-1 p-Br-Ph H H H ⁿ Bu Och ₃ F F OH H H XIX-39-2 p-Br-Ph H H CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-39-8 p-Br-Ph * H * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-40-1 p-1-ph N N n ⁿ Bu Och ₃ F F OH H H XIX-40-2 p-1-ph N N CH ₃ ⁿ Bu Och ₃ F F OH H H XIX-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-40-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ F F OH H H XIX-40-5 p-1-ph N N CH ₂ Ph ⁿ Bu Och ₃ F F OH H H XIX-40-6 p-1-ph N N CH ₂ -indol-3-yl ⁿ Bu Och ₃ F F OH H H XIX-40-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ F F OH H H XIX-40-8 p-1-ph * n * ⁿ Bu Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-41-1 CH ₃ N n n Bz Och ₃ F F OH H H XIX-41-2 CH ₃ N n CH ₃ Bz Och ₃ F F OH H H XIX-41-3 CH ₃ n n CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-41-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-41-5 CH ₃ n n CH ₂ Ph Bz Och ₃ F F OH H H XIX-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-41-8 CH ₃ * n * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-42-1 Et H H H Bz Och ₃ F F OH H H XIX-42-2 Et H H CH ₃ Bz Och ₃ F F OH H H XIX-42-3 Et H H CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-42-5 Et H H CH ₂ Ph Bz Och ₃ F F OH H H XIX-42-6 Et H H CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-42-8 Et * H * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-43-1 ⁱ Pr N n n Bz Och ₃ F F OH H H XIX-43-2 ⁱ Pr N n CH ₃ Bz Och ₃ F F OH H H XIX-43-3 ⁱ Pr n n CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-43-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-43-5 ⁱ Pr n n CH ₂ Ph Bz Och ₃ F F OH H H XIX-43-6 ⁱ Pr n n CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-43-8 ⁱ Pr * n * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-44-1 ^t Bu N N N Bz Och ₃ F F OH H H XIX-44-2 ^t Bu N N CH ₃ Bz Och ₃ F F OH H H XIX-44-3 ^t Bu N N CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-44-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-44-5 ^t Bu N N CH ₂ Ph Bz Och ₃ F F OH H H XIX-44-6 ^t Bu N N CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-44-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-44-8 ^t Bu * N * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-45-1 Ph H H H Bz Och ₃ F F OH H H XIX-45-2 Ph H H CH ₃ Bz Och ₃ F F OH H H XIX-45-3 Ph H H CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-45-5 Ph H H CH ₂ Ph Bz Och ₃ F F OH H H XIX-45-6 Ph H H CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-45-8 Ph * H * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-46-1 p-me-ph H H H Bz Och ₃ F F OH H H XIX-46-2 p-me-ph H H CH ₃ Bz Och ₃ F F OH H H XIX-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-46-5 p-me-ph H H CH ₂ Ph Bz Och ₃ F F OH H H XIX-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-46-8 p-me-ph * H * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-47-1 p-f-ph H H H Bz Och ₃ F F OH H H XIX-47-2 p-f-ph H H CH ₃ Bz Och ₃ F F OH H H XIX-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-47-5 p-f-ph H H CH ₂ Ph Bz Och ₃ F F OH H H XIX-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-47-8 p-f-ph * H * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-48-1 p-Cl-Ph H H H Bz Och ₃ F F OH H H XIX-48-2 p-Cl-Ph H H CH ₃ Bz Och ₃ F F OH H H XIX-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H Hgh-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-48-5 p-Cl-Ph H H CH ₂ Ph Bz Och ₃ F F OH H H XIX-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-48-8 p-Cl-Ph * H * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XIX-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-49-1 p-Br-Ph H H H Bz Och ₃ F F OH H H XIX-49-2 p-Br-Ph H H CH ₃ Bz Och ₃ F F OH H H XIX-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-49-5 p-Br-Ph H H CH ₂ Ph Bz Och ₃ F F OH H H XIX-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-49-8 p-Br-Ph * H Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XIX-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XIX-50-1 p-1-ph N N n Bz Och ₃ F F OH H H XIX-50-2 p-1-ph N N CH ₃ Bz Och ₃ F F OH H H XIX-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-50-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ F F OH H H XIX-50-5 p-1-ph N n CH ₂ Ph Bz Och ₃ F F OH H H XIX-50-6 p-1-ph n n CH ₂ -indol-3-yl Bz Och ₃ F F OH H H XIX-50-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ Bz Och ₃ F F OH H H XIX-50-8 p-1-ph * n * Bz Och ₃ F F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-1-1 CH ₃ N N n CH ₃ OCH ₃ N F IT N n XX-1-2 CH ₃ N N CH ₃ CH ₃ OCH ₃ N F IT N n XX-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT N n XX-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT N n XX-1-5 CH ₃ N n CH ₂ Ph CH ₃ OCH ₃ N F IT N n XX-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ OCH ₃ N F IT N n XX-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ N F IT N n XX-1-8 CH ₃ * n * CH ₃ OCH ₃ N F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-2-1 Et H H H CH ₃ OCH ₃ N F IT N N XX-2-2 Et H H CH ₃ CH ₃ OCH ₃ N F IT N N XX-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ n F IT N n XX-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ n F IT N n XX-2-5 Et H H CH ₂ Ph CH ₃ OCH ₃ n F IT N n XX-2-6 Et H H CH ₂ -indol-3-yl CH ₃ OCH ₃ n F IT N n XX-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ n F IT n n XX-2-8 Et * H * CH ₃ OCH ₃ n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-3-1 ⁱ Pr H H H CH ₃ OCH ₃ N F IT n n XX-3-2 ⁱ Pr H H CH ₃ CH ₃ OCH ₃ N F IT n n XX-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ OCH ₃ N F IT n n XX-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ OCH ₃ n F IT n n XX-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ n F IT n n XX-3-8 ⁱ Pr * H CH ₃ OCH ₃ n F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-4-1 ^t Bu N N n CH ₃ OCH ₃ N F IT N N XX-4-2 ^t Bu N N CH ₃ CH ₃ OCH ₃ S F IT N N XX-4-3 ^t Bu N N CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n N XX-4-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n N XX-4-5 ^t Bu N n CH ₂ Ph CH ₃ OCH ₃ N F IT n n XX-4-6 ^t Bu n n CH ₂ -indol-3-yl CH ₃ OCH ₃ N F IT n n XX-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ N F IT n n XX-4-8 ^t Bu * n * CH ₃ OCH ₃ N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-5-1 Ph H H H CH ₃ OCH ₃ N F IT N n XX-5-2 Ph H H CH ₃ CH ₃ OCH ₃ N F IT N n XX-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-5-5 Ph H H CH ₂ Ph CH ₃ OCH ₃ N F IT n n XX-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ N F IT n n XX-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ N F IT n n XX-5-8 Ph * H * CH ₃ OCH ₃ N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-6-1 p-me-ph H H H CH ₃ OCH ₃ N F IT N N XX-6-2 p-me-ph H H CH ₃ CH ₃ OCH ₃ N F IT N N XX-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT N n XX-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT N n XX-6-5 p-me-ph H H CH ₂ Ph CH ₃ OCH ₃ n F IT N n XX-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ n F IT N n XX-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ n F IT N n XX-6-8 p-me-ph * H * CH ₃ OCH ₃ n F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-7-1 p-f-ph H H H CH ₃ OCH ₃ N F IT N n XX-7-2 p-f-ph H H CH ₃ CH ₃ OCH ₃ N F IT n n XX-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-7-6 p-f-ph H H CH ₂ Ph CH ₃ OCH ₃ N F IT n n XX-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ N F IT n n XX-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ N F IT n n XX-7-20 p-f-ph * H * CH ₃ OCH ₃ N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-8-1 p-Cl-Ph H H H CH ₃ OCH ₃ N F IT N N XX-8-2 p-Cl-Ph H H CH ₃ CH ₃ OCH ₃ N F IT N N XX-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n N XX-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ n F IT n N XX-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ OCH ₃ n F IT n n XX-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ n F IT n n XX-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ n F IT n n XX-8-8 p-Cl-Ph * H * CH ₃ OCH ₃ n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-9-1 p-Br-Ph H H H CH ₃ OCH ₃ N F IT n N XX-9-2 p-Br-Ph H H CH ₃ CH ₃ OCH ₃ N F IT n N XX-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n n XX-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ OCH ₃ N F IT n n XX-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ OCH ₃ N F it n n XX-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ N F it n n XX-9-20 p-Br-Ph * H * CH ₃ OCH ₃ N F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-10-1 p-1-ph n n n CH ₃ OCH ₃ N F IT N N XX-10-2 p-1-ph N n CH ₃ CH ₃ OCH ₃ N F IT N N XX-10-3 p-1-ph n n CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n N XX-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ OCH ₃ N F IT n N XX-10-5 p-1-ph N n CH ₂ Ph CH ₃ OCH ₃ N F IT n n XX-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ OCH ₃ N F IT n n XX-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ OCH ₃ N F IT n n XX-10-8 p-1-ph * n * CH ₃ OCH ₃ N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-11-1 CH ₃ N N n Et Och ₃ N F IT n n XX-11-2 CH ₃ N N CH ₃ Et Och ₃ N F IT n n XX-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et OCH ₃ N F IT n n XX-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et OCH ₃ N F IT n n XX-11-5 CH ₃ N n CH ₂ Ph Et OCH ₃ N F IT n n XX-11-6 CH ₃ N n CH ₂ -indol-3-yl Et OCH ₃ N F IT n n XX-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et OCH ₃ N F it n n XX-11-8 CH ₃ * n * Et OCH ₃ N F it n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-12-1 Et H H H Et Och ₃ H F OH H H XX-12-2 Et H H CH ₃ Et Och ₃ H F OH H H XX-12-3 Et H H CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-12-5 Et H H CH ₂ Ph Et Och ₃ H F OH H H XX-12-6 Et H H CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-12-8 Et * H * Et Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-13-1 ⁱ Pr N N n Et Och ₃ H F OH H H XX-13-2 ⁱ Pr N N CH ₃ Et Och ₃ H F OH H H XX-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-13-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-13-5 ⁱ Pr N n CH ₂ Ph Et Och ₃ H F OH H H XX-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-13-8 ⁱ Pr * n * Et Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R XX-14-1 ^t Bu N N n Et Och ₃ H F OH H H XX-14-2 ^t Bu N N CH ₃ Et Och ₃ H F OH H H XX-14-3 ^t Bu N N CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-14-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-14-5 ^t Bu N N CH ₂ Ph Et Och ₃ H F OH H H XX-14-6 ^t Bu N N CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-14-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-14-8 ^t Bu * N * Et Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-15-1 Ph H H H Et Och ₃ H F OH H H XX-15-2 Ph H H CH ₃ Et Och ₃ H F OH H H XX-15-3 Ph H H CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-15-5 Ph H H CH ₂ Ph Et Och ₃ H F OH H H XX-15-6 Ph H H CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-15-8 Ph * H * Et Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-16-1 p-me-ph H H H Et Och ₃ H F IT N N XX-16-2 p-me-ph H H CH ₃ Et Och ₃ H F IT N n XX-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et Och ₃ N F IT N n XX-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ N F IT N n XX-16-5 p-me-ph H H CH ₂ Ph Et Och ₃ N F IT N n XX-16-6 p-me-ph H H CH ₂ -indol-3-yl Et Och ₃ N F IT N n XX-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ N F IT N n XX-16-8 p-me-ph * H * Et Och ₃ N F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-17-1 p-f-ph H H H Et OCH ₃ N F IT N n XX-17-2 p-f-ph H H CH ₃ Et Och ₃ N F IT N n XX-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et Och ₃ N F IT N n XX-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et OCH ₃ N F IT N n XX-17-5 p-f-ph H H CH ₂ Ph Et OCH ₃ N F IT n n XX-17-6 p-f-ph H H CH ₂ -indol-3-yl Et OCH ₃ N F IT n n XX-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et OCH ₃ N F IT n n XX-17-8 p-f-ph * H * Et OCH ₃ N F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-18-1 p-Cl-Ph H H H Et Och ₃ H F OH H H XX-18-2 p-Cl-Ph H H CH ₃ Et Och ₃ H F OH H H XX-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-18-5 p-Cl-Ph H H CH ₂ Ph Et Och ₃ H F OH H H XX-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-18-8 p-Cl-Ph * H * Et Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-19-1 p-Br-Ph H H H Et Och ₃ H F OH H H XX-19-2 p-Br-Ph H H CH ₃ Et Och ₃ H F OH H H XX-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-19-5 p-Br-Ph H H CH ₂ Ph Et Och ₃ H F OH H H XX-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-19-8 p-Br-Ph * H * Et Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-20-1 p-1-ph N N n Et Och ₃ H F OH H H XX-20-2 p-1-ph N N CH ₃ Et Och ₃ H F OH H H XX-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et Och ₃ H F OH H H XX-20-5 p-1-ph N n CH ₂ Ph Et Och ₃ H F OH H H XX-20-6 p-1-ph N n CH ₂ -indol-3-yl Et Och ₃ H F OH H H XX-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et Och ₃ H F OH H H XX-20-8 p-1-ph * n * Et OCH ₃ , H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-21-1 CH ₃ N n n ⁱ Pr OCH ₃ N F IT N N XX-21-2 CH ₃ N n CH ₃ ⁱ Pr OCH ₃ N F IT N N XX-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N n XX-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N n XX-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr OCH ₃ N F IT N n XX-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ N F IT N n XX-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ N F IT N n XX-21-8 CH ₃ * n * ⁱ Pr OCH ₃ N F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-22-1 Et H H H ⁱ Pr Och ₃ H F OH H H XX-22-2 Et H H CH ₃ ⁱ Pr Och ₃ H F OH H H XX-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-22-5 Et H H CH ₂ Ph ⁱ Pr Och ₃ H F OH H H XX-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ H F OH H H XX-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ H F OH H H XX-22-8 Et * H * ⁱ Pr Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-23-1 ⁱ Pr N N N ⁱ Pr OCH ₃ N F IT N N XX-23-2 ⁱ Pr N N CH ₃ ⁱ Pr OCH ₃ N F IT N n XX-23-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N n XX-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N n XX-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr OCH ₃ N F IT N n XX-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ N F IT N n XX-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ n F IT N n XX-23-8 ⁱ Pr * n * ⁱ Pr OCH ₃ n F IT N n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-24-1 ^t Bu N N n ⁱ Pr OCH ₃ N F IT N n XX-24-2 ^t Bu n N CH ₃ ⁱ Pr OCH ₃ N F IT N n XX-24-3 ^t Bu N N CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ n F IT n n XX-24-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ n F IT n n XX-24-5 ^t Bu N n CH ₂ Ph ⁱ Pr OCH ₃ n F IT n n XX-24-6 ^t Bu N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ n F IT n n XX-24-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ n F IT n n XX-24-8 ^t Bu * n * ⁱ Pr OCH ₃ n F IT n n * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-25-1 Ph H H H ⁱ Pr Och ₃ H F OH H H XX-25-2 Ph H H CH ₃ ⁱ Pr Och ₃ H F OH H H XX-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-25-5 Ph H H CH ₂ Ph ⁱ Pr Och ₃ H F OH H H XX-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ H F OH H H XX-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ H F OH H H XX-25-8 Ph * H * ⁱ Pr Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-26-1 p-me-ph H H H ⁱ Pr OCH ₃ N F IT N N XX-26-2 p-me-ph H H CH ₃ ⁱ Pr Och ₃ N F IT N N XX-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N N XX-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N N XX-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr OCH ₃ N F IT N N XX-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr OCH ₃ N F IT N N XX-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ N F IT N N XX-26-8 p-me-ph * H * ⁱ Pr OCH ₃ N F IT n N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-27-1 p-f-ph H H H ⁱ Pr Och ₃ H F OH H H XX-27-2 p-f-ph H H CH ₃ ⁱ Pr Och ₃ H F OH H H XX-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr Och ₃ H F OH H H XX-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ H F OH H H XX-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ H F OH H H XX-27-8 p-f-ph * H * ⁱ Pr Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-28-1 p-Cl-Ph H H H ⁱ Pr Och ₃ H F OH H H XX-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr Och ₃ H F OH H H XX-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr Och ₃ H F OH H H XX-28-6 p-CI-Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ H F OH H H XX-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ H F OH H H XX-28-8 p-Cl-Ph * H * ⁱ Pr Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-29-1 p-Br-Ph H H H ⁱ Pr Och ₃ H F OH H H XX-29-2 p-Br-Ph H H CH ₃ ⁱ Pr Och ₃ H F OH H H XX-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr Och ₃ H F OH H H XX-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr Och ₃ H F OH H H XX-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr Och ₃ H F OH H H XX-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr Och ₃ H F OH H H XX-29-8 p-Br-Ph * H * ⁱ Pr Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-30-1 p-1-ph N n n ⁱ Pr OCH ₃ N F IT N N XX-30-2 p-1-ph N n CH ₃ ⁱ Pr OCH ₃ N F IT N N XX-30-3 p-1-ph N n CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N N XX-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr OCH ₃ N F IT N N XX-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr OCH ₃ N F IT N N XX-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr OCH ₃ N F IT N N XX-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr OCH ₃ N F IT N N XX-30-8 p-1-ph n ⁱ Pr OCH ₃ N F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-31-1 CH ₃ N n n ⁿ Bu Och ₃ H F OH H H XX-31-2 CH ₃ N n CH ₃ ⁿ Bu Och ₃ H F OH H H XX-31-3 CH ₃ n n CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-31-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-31-5 CH ₃ n n CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-31-6 CH ₃ n n CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-31-8 CH ₃ * n * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-32-1 Et H H H ⁿ Bu Och ₃ H F OH H H XX-32-2 Et H H CH ₃ ⁿ Bu Och ₃ H F OH H H XX-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-32-5 Et H H CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-32-8 Et * H * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-33-1 ⁱ Pr N N n ⁿ Bu Och ₃ H F OH H H XX-33-2 ⁱ Pr N N CH ₃ ⁿ Bu Och ₃ H F OH H H XX-33-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-33-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-33-5 ⁱ Pr N n CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-33-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-33-8 ⁱ Pr * n * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-34-1 ^t Bu N N N ⁿ Bu OCH ₃ N F IT N N XX-34-2 ^t Bu N N CH ₃ ⁿ Bu OCH ₃ N F IT N N XX-34-3 ^t Bu N N CH (CH ₃ ) ₂ ⁿ Bu OCH ₃ N F IT N N XX-34-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu OCH ₃ N F IT N N XX-34-5 ^t Bu N N CH ₂ Ph ⁿ Bu OCH ₃ N F IT N N XX-34-6 ^t Bu N N CH ₂ -indol-3-yl ⁿ Bu OCH ₃ N F IT N N XX-34-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ ⁿ Bu OCH ₃ n F IT N N XX-34-8 ^t Bu * N * ⁿ Bu OCH ₃ n F IT N N * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-35-1 Ph H H H ⁿ Bu Och ₃ H F OH H H XX-35-2 Ph H H CH ₃ ⁿ Bu Och ₃ H F OH H H XX-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-35-5 Ph H H CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-35-8 Ph * H * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-36-1 p-me-ph H H H ⁿ Bu Och ₃ H F OH H H XX-36-2 p-me-ph H H CH ₃ ⁿ Bu Och ₃ H F OH H H XX-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-36-8 p-me-ph * H * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-37-1 p-f-ph H H H ⁿ Bu Och ₃ H F OH H H XX-37-2 p-f-ph H H CH ₃ ⁿ Bu Och ₃ H F OH H H XX-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-37-8 p-f-ph * H * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-38-1 p-Cl-Ph H H H ⁿ Bu Och ₃ H F OH H H XX-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu Och ₃ H F OH H H XX-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-38-8 p-CI-Ph * H * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-39-1 p-Br-Ph H H H ⁿ Bu Och ₃ H F OH H H XX-39-2 p-Br-Ph H H CH ₃ ⁿ Bu Och ₃ H F OH H H XX-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-39-8 p-Br-Ph * H * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-40-1 p-1-ph N n n ⁿ Bu Och ₃ H F OH H H XX-40-2 p-1-ph N n CH ₃ ⁿ Bu Och ₃ H F OH H H XX-40-3 p-1-ph n n CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-40-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu Och ₃ H F OH H H XX-40-5 p-1-ph n n CH ₂ Ph ⁿ Bu Och ₃ H F OH H H XX-40-6 p-1-ph n n CH ₂ -indol-3-yl ⁿ Bu Och ₃ H F OH H H XX-40-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁿ Bu Och ₃ H F OH H H XX-40-8 p-1-ph * n * ⁿ Bu Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-41-1 CH ₃ N N n Bz Och ₃ H F OH H H XX-41-2 CH ₃ N N CH ₃ Bz Och ₃ H F OH H H XX-41-3 CH ₃ n N CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-41-4 CH ₃ n N CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-41-5 CH ₃ n N CH ₂ Ph Bz Och ₃ H F OH H H XX-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-41-8 CH ₃ * n * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-42-1 Et H H H Bz Och ₃ H F OH H H XX-42-2 Et H H CH ₃ Bz Och ₃ H F OH H H XX-42-3 Et H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-42-5 Et H H CH ₂ Ph Bz Och ₃ H F OH H H XX-42-6 Et H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-42-8 Et * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-43-1 ⁱ Pr N n n Bz Och ₃ H F OH H H XX-43-2 ⁱ Pr N n CH ₃ Bz Och ₃ H F OH H H XX-43-3 ⁱ Pr N n CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-43-5 ⁱ Pr N n CH ₂ Ph Bz Och ₃ H F OH H H XX-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-43-8 ⁱ Pr * n * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-44-1 ^t Bu H H H Bz OCH ₃ H F OH H H XX-44-2 ^t Bu H H CH ₃ Bz Och ₃ H F OH H H XX-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz Och H F OH H H XX-44-5 ^t Bu H H CH ₂ Ph Bz Och ₃ H F OH H H XX-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-44-8 ^t Bu * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-45-1 Ph H H H Bz Och ₃ H F OH H H XX-45-2 Ph H H CH ₃ Bz Och ₃ H F OH H H XX-45-3 Ph H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-45-5 Ph H H CH ₂ Ph Bz Och ₃ H F OH H H XX-45-6 Ph H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-45-8 Ph * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-46-1 p-me-ph H H H Bz Och ₃ H F OH H H XX-46-2 p-me-ph H H CH ₃ Bz Och ₃ H F OH H H XX-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-46-5 p-me-ph H H CH ₂ Ph Bz Och H F OH H H XX-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-46-8 p-me-ph * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-47-1 p-f-ph H H H Bz Och ₃ H F OH H H XX-47-2 p-f-ph H H CH ₃ Bz Och ₃ H F OH H H XX-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-47-5 p-f-ph H H CH ₂ Ph Bz Och ₃ H F OH H H XX-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-47-8 p-f-ph * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-48-1 p-Cl-Ph H H H Bz Och ₃ H F OH H H XX-48-2 p-Cl-Ph H H CH ₃ Bz Och ₃ H F OH H H XX-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-48-5 p-Cl-Ph H H CH ₂ Ph Bz Och ₃ H F OH H H XX-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-48-8 p-Cl-Ph * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XX-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-49-1 p-Br-Ph H H H Bz Och ₃ H F OH H H XX-49-2 p-Br-Ph H H CH ₃ Bz Och ₃ H F OH H H XX-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-49-5 p-Br-Ph H H CH ₂ Ph Bz Och ₃ H F OH H H XX-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-49-8 p-Br-Ph * H * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XX-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y R ⁷ R ⁸ XX-50-1 p-1-ph N N n Bz Och ₃ H F OH H H XX-50-2 p-1-ph N N CH ₃ Bz Och ₃ H F OH H H XX-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-50-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Bz Och ₃ H F OH H H XX-50-5 p-1-ph N N CH ₂ Ph Bz Och ₃ H F OH H H XX-50-6 p-1-ph N N CH ₂ -indol-3-yl Bz Och ₃ H F OH H H XX-50-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Bz Och ₃ H F OH H H XX-50-8 p-1-ph * n * Bz Och ₃ H F OH H H * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-1-1 CH ₃ N n n CH ₃ N CH ₃ F IT XXI-1-2 CH ₃ N n CH ₃ CH ₃ N CH ₃ F IT XXI-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-1-5 CH ₃ N n CH ₂ Ph CH ₃ N CH ₃ F IT XXI-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXI-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT XXI-1-8 CH ₃ * n * CH ₃ N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-2-1 Et N n n CH ₃ N CH ₃ F IT

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-2-2 Et H H CH ₃ CH ₃ H CH ₃ F OH XXI-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXI-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXI-2-5 Et H H CH ₂ Ph CH ₃ H CH ₃ F OH XXI-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXI-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXI-2-8 Et * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-3-1 ⁱ Pr N n n CH ₃ N CH ₃ F IT XXI-3-2 ⁱ Pr N n sun ₃ sun ₃ N CH ₃ F IT XXI-3-3 ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXI-3-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXI-3-5 ⁱ Pr n n CH ₂ Ph CH ₃ n CH ₃ F IT XXI-3-6 ⁱ Pr n n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXI-3-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXI-3-8 ⁱ Pr * n * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-4-1 ^t Bu N n n CH ₃ N CH ₃ F IT XXI-4-2 ^t Bu N n CH ₃ CH ₃ N CH ₃ F IT XXI-4-3 ^t Bu N n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-4-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-4-5 ^t Bu n n CH ₂ Ph CH ₃ N CH ₃ F IT XXI-4-6 ^t Bu n n CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXI-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXI-4-8 ^t Bu * n * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-5-1 Ph H H H CH ₃ n CH ₃ F IT XXI-5-2 Ph H H CH ₃ CH ₃ n CH ₃ F IT XXI-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXI-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXI-5-5 Ph H H CH ₂ Ph CH ₃ n CH ₃ F IT XXI-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXI-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXI-5-8 Ph * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-6-1 p-me-ph H H H CH ₃ N CH ₃ F IT XXI-6-2 p-me-ph H H CH ₃ CH ₃ N CH ₃ F IT XXI-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-6-5 p-me-ph H H CH ₂ Ph CH ₃ N CH ₃ F IT XXI-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXI-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXI-6-8 p-me-ph * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-7-1 p-f-ph H H H CH ₃ N CH ₃ F IT XXI-7-2 p-f-ph H H CH ₃ CH ₃ N CH ₃ F IT XXI-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXI-7-6 p-f-ph H H CH ₂ Ph CH ₃ N CH ₃ F IT XXI-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXI-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT XXI-7-20 p-f-ph * H * CH ₃ N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-8-1 p-Cl-Ph H H H CH ₃ H CH ₃ F OH XXI-8-2 p-Cl-Ph H H CH ₃ CH ₃ H CH ₃ F OH XXI-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXI-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXI-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ H CH ₃ F OH XXI-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXI-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXI-8-8 p-Cl-Ph * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-9-1 p-Br-Ph H H H CH ₃ H CH ₃ F OH XXI-9-2 p-Br-Ph H H CH ₃ CH ₃ H CH ₃ F OH XXI-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXI-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXI-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ H CH ₃ F OH XXI-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXI-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXI-9-20 p-Br-Ph * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-10-1 p-1-ph N N n sun ₃ n CH ₃ F IT XXI-10-2 p-1-ph N N sun ₃ CH ₃ n CH ₃ F IT XXI-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXI-10-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXI-10-5 p-1-ph N N CH ₂ Ph CH ₃ n CH ₃ F IT XXI-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXI-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXI-10-8 p-1-ph * n * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-11-1 CH ₃ H H H Et H CH ₃ F IT XXI-11-2 CH ₃ H H CH ₃ Et H CH ₃ F IT XXI-11-3 CH ₃ H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-11-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-11-5 CH ₃ H H CH ₂ Ph Et H CH ₃ F IT XXI-11-6 CH ₃ H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-11-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-11-8 CH ₃ * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-12-1 Et H H H Et H CH ₃ F IT XXI-12-2 Et H H CH ₃ Et H CH ₃ F IT XXI-12-3 Et H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-12-5 Et H H CH ₂ Ph Et H CH ₃ F IT XXI-12-6 Et H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-12-8 Et * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-13-1 ⁱ Pr N N N Et H CH ₃ F IT XXI-13-2 ⁱ Pr n N CH ₃ Et H CH ₃ F IT XXI-13-3 ⁱ Pr n N CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-13-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-13-5 ⁱ Pr N N CH ₂ Ph Et H CH ₃ F IT XXI-13-6 ⁱ Pr N N CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-13-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-13-8 ⁱ Pr * N * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-14-1 ^t Bu N N n Et H CH ₃ F IT XXI-14-2 ^t Bu N N CH ₃ Et H CH ₃ F IT XXI-14-3 ^t Bu N N CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-14-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-14-5 ^t Bu N n CH ₂ Ph Et H CH ₃ F IT XXI-14-6 ^t Bu N n CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-14-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-14-8 ^t Bu * n * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-15-1 Ph H H H Et H CH ₃ F IT XXI-15-2 Ph H H CH ₃ Et H CH ₃ F IT XXI-15-3 Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-15-5 Ph H H CH ₂ Ph Et H CH ₃ F IT XXI-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-15-8 Ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-16-1 p-me-ph H H H Et H CH ₃ F IT XXI-16-2 p-me-ph H H CH ₃ Et H CH ₃ F IT XXI-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-16-5 p-me-ph H H CH ₂ Ph Et H CH ₃ F IT XXI-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-16-8 p-me-ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-17-1 p-f-ph H H H Et H CH ₃ F IT XXI-17-2 p-f-ph H H CH ₃ Et H CH ₃ F IT XXI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ F IT XXI-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-17-8 p-f-ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-18-1 p-Cl-Ph H H H Et H CH ₃ F IT XXI-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ F IT XXI-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F it XXI-18-5 p-Cl-Ph H H CH ₂ Ph Et H CH ₃ F it XXI-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F it XXI-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F it XXI-18-8 p-Cl-Ph * H * Et H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-19-1 p-Br-Ph H H H Et H CH ₃ F IT XXI-19-2 p-Br-Ph H H CH ₃ Et H CH ₃ F IT XXI-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-19-5 p-Br-Ph H H CH ₂ Ph Et H CH ₃ F IT XXI-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-19-8 p-Br-Ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-20-1 p-1-ph N N n Et H CH ₃ F IT XXI-20-2 p-1-ph N N CH ₃ Et H CH ₃ F IT XXI-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXI-20-5 p-1-ph n N CH ₂ Ph Et H CH ₃ F IT XXI-20-6 p-1-ph n N CH ₂ -indol-3-yl Et H CH ₃ F IT XXI-20-7 p-1-ph n N CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXI-20-8 p-1-ph * n * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-21-1 CH ₃ N N n ⁱ Pr N CH ₃ F IT XXI-21-2 CH ₃ N N CH ₃ ⁱ Pr N CH ₃ F IT XXI-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXI-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXI-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr n CH ₃ F IT XXI-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT XXI-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT XXI-21-8 CH ₃ * n * ⁱ Pr n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-22-1 Et H H H ⁱ Pr H CH ₃ F IT XXI-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ F IT XXI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXI-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXI-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXI-22-8 Et * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-23-1 ⁱ Pr N N n ⁱ Pr N CH ₃ F IT XXI-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N CH ₃ F IT XXI-23-3 ⁱ Pr n N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXI-23-4 ⁱ Pr n N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXI-23-5 ⁱ Pr n n CH ₂ Ph ⁱ Pr N CH ₃ F IT XXI-23-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT XXI-23-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT XXI-23-8 ⁱ Pr * n * ⁱ Pr N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-24-1 ^t Bu N n n ⁱ Pr N CH ₃ F IT XXI-24-2 ^t Bu N n CH ₃ ⁱ Pr N CH ₃ F IT XXI-24-3 ^t Bu N n CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXI-24-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXI-24-5 ^t Bu N n CH ₂ Ph ⁱ Pr n CH ₃ F IT XXI-24-6 ^t Bu N n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT XXI-24-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT XXI-24-8 ^t Bu * n * ⁱ Pr n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-2S-1 Ph H H H ⁱ Pr H CH ₃ F IT XXI-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXI-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXI-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXI-25-8 Ph * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-26-1 p-me-ph H H H ⁱ Pr H CH ₃ F IT XXI-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXI-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXI-26-8 p-me-ph * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-27-1 p-f-ph H H H ⁱ Pr H CH ₃ F IT XXI-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXI-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXI-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXI-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXI-27-8 p-f-ph * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-28-1 p-Cl-Ph H H H ⁱ Pr H CH ₃ F IT XXI-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXI-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXI-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXI-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXI-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXI-28-8 p-Cl-Ph * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ F OH XXI-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXI-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXI-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXI-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXI-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXI-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXI-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ F OH * R2 and Rib are connected to each other via (CH ₂ ) s to form a five-membered ring. Table XXI-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-30-1 p-1-ph N N N ⁱ Pr N CH ₃ F IT XXI-30-2 p-1-ph N n CH ₃ ⁱ Pr N CH ₃ F IT XXI-30-3 p-1-ph N n CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXI-30-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXI-30-5 p-1-ph n n CH ₂ Ph ⁱ Pr n CH ₃ F IT XXI-30-6 p-1-ph n n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT XXI-30-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT XXI-30-8 p-1-ph * n * ⁱ Pr n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-31-1 CH ₃ N N N ⁿ Bu H CH ₃ F IT XXI-31-2 CH ₃ N n CH ₃ ⁿ Bu H CH ₃ F IT XXI-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-31-8 CH ₃ * N * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-32-1 Et H H H ⁿ Bu H CH ₃ F IT XXI-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ F IT XXI-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-32-8 Et * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-33-1 ⁱ Pr N n n ⁿ Bu H CH ₃ F IT XXI-33-2 ⁱ Pr N n CH ₃ ⁿ Bu H CH ₃ F IT XXI-33-3 ⁱ Pr n n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-33-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-33-5 ⁱ Pr n n CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-33-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-33-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-33-8 ⁱ Pr * n ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-34-1 ^t Bu N n n ⁿ Bu N CH ₃ F IT XXI-34-2 ^t Bu n n CH ₃ ⁿ Bu N CH ₃ F IT XXI-34-3 ^t Bu n n CH (CH ₃ ) ₂ ⁿ Bu N CH ₃ F IT XXI-34-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N CH ₃ F IT XXI-34-5 ^t Bu n n CH ₂ Ph ⁿ Bu N CH ₃ F IT XXI-34-6 ^t Bu n n CH ₂ -indol-3-yl ⁿ Bu n CH ₃ F IT XXI-34-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ ⁿ Bu n CH ₃ F IT XXI-34-8 ^t Bu * n * ⁿ Bu n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-35-1 Ph H H H ⁿ Bu H CH ₃ F IT XXI-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXI-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-35-8 Ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-36-1 p-me-ph H H H ⁿ Bu H CH ₃ F IT XXI-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXI-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F it XXI-36-8 p-me-ph * H * ⁿ Bu H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-37-1 p-f-ph H H H ⁿ Bu H CH ₃ F IT XXI-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXI-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-37-8 p-f-ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ F IT XXI-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXI-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-38-8 p-Cl-Ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ F IT XXI-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXI-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXI-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-40-1 p-1-ph N n n ⁿ Bu H CH ₃ F IT XXI-40-2 p-1-ph N n CH ₃ ⁿ Bu H CH ₃ F IT XXI-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXI-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H CH ₃ F IT XXI-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXI-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F it XXI-40-8 p-1-ph * n * ⁿ Bu H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-41-1 CH ₃ N n n Bz H CH ₃ F IT XXI-41-2 CH ₃ N n CH ₃ Bz H CH ₃ F IT XXI-41-3 CH ₃ n n CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-41-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-41-5 CH ₃ n n CH ₂ Ph Bz H CH ₃ F it XXI-41-6 CH ₃ n n CH ₂ -indol-3-yl Bz H CH ₃ F it XXI-41-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F it XXI-41-8 CH ₃ * n * Bz H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-42-1 Et H H H Bz H CH ₃ F IT XXI-42-2 Et H H CH ₃ Bz H CH ₃ F IT XXI-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-42-5 Et H H CH ₂ Ph Bz H CH ₃ F IT XXI-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-42-8 Et * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-43-1 ⁱ Pr N N n Bz H CH ₃ F IT XXI-43-2 ⁱ Pr N N CH ₃ Bz H CH ₃ F IT XXI-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F it XXI-43-5 ⁱ Pr N n CH ₂ Ph Bz H CH ₃ F it XXI-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz H CH ₃ F it XXI-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F it XXI-43-8 ⁱ Pr * n * Bz H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-44-1 ^t Bu N n n Bz H CH ₃ F IT XXI-44-2 ^t Bu N n CH ₃ Bz H CH ₃ F IT XXI-44-3 ^t Bu N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-44-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-44-5 ^t Bu N n CH ₂ Ph Bz H CH ₃ F IT XXI-44-6 ^t Bu n n CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-44-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-44-8 ^t Bu * n * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-45-1 Ph H H H Bz H CH ₃ F IT XXI-45-2 Ph H H CH ₃ Bz H CH ₃ F IT XXI-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-45-5 Ph H H CH ₂ Ph Bz H CH ₃ F IT XXI-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-45-8 Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-46-1 p-me-ph H H H Bz H CH ₃ F IT XXI-46-2 p-me-ph H H CH ₃ Bz H CH ₃ F IT XXI-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ F IT XXI-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-46-8 p-me-ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-47-1 p-f-ph H H H Bz H CH ₃ F IT XXI-47-2 p-f-ph H H CH ₃ Bz H CH ₃ F IT XXI-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ F IT XXI-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-47-8 p-f-ph * H * Bz H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-48-1 p-Cl-Ph H H H Bz H CH ₃ F IT XXI-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ F IT XXI-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ F IT XXI-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-48-8 p-Cl-Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXI-49. No. R R R3a Rib R Rj R X Y XXI-49-1 p-Br-Ph H H H Bz H CH ₃ F IT XXI-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ F IT XXI-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ F IT XXI-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-49-8 p-Br-Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXI-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXI-50-1 p-1-ph N N n Bz H CH ₃ F IT XXI-50-2 p-1-ph N N CH ₃ Bz H CH ₃ F IT XXI-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXI-50-5 p-1-ph N n CH ₂ Ph Bz H CH ₃ F IT XXI-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H CH ₃ F IT XXI-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXI-50-8 p-1-ph * n * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y HHP-1-1 CH ₃ N n n CH ₃ N F N IT HHP-1-2 CH ₃ N n CH ₃ CH ₃ n F N IT HHP-1-3 CH ₃ n n CH (CH ₃ ) ₂ CH ₃ n F N IT XXII-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT XXII-1-5 CH ₃ n n CH ₂ Ph CH ₃ n F N IT XXII-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ n F N IT XXII-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT HHP-1-8 CH ₃ * n * CH ₃ n F N it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-2-1 Et H H H CH ₃ N F n IT XXII-2-2 Et H H CH ₃ CH ₃ N F n it XXII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N F n it XXII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXII-2-5 Et H H CH ₂ Ph CH ₃ N F n it XXII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N F n it XXII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it XXII-2-8 Et * H * CH ₃ N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-3-1 ⁱ Pr N N n CH ₃ n F n IT HHP-3-2 ⁱ Pr N N CH ₃ CH ₃ n F n IT ХХП-3-З ⁱ Pr n N CH (CH ₃ ) ₂ CH ₃ n F n it HHP-3-4 ⁱ Pr n N CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it XXII-3-5 ⁱ Pr n N CH ₂ Ph CH ₃ n F n it XXII-3-6 ⁱ Pr n n CH ₂ -indol-3-yl CH ₃ n F n it XHI-3-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXII-3-8 ⁱ Pr * n * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-4-1 ^t Bu N n n CH ₃ N F n IT HHP-4-2 ^t Bu N n CH ₃ CH ₃ N F n IT HHP-4-3 ^t Bu n n CH (CH ₃ ) ₂ CH ₃ N F n it HHP-4-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it HHP-4-5 ^t Bu n n CH ₂ Ph CH ₃ N F n it HHP-4-6 ^t Bu n n CH ₂ -indol-3-yl CH ₃ N F n it XXII-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ N F n it XXII-4-8 ^t Bu * n * CH ₃ N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-5-1 Ph H H H CH ₃ N F n IT XXII-5-2 Ph H H CH ₃ CH ₃ N F n IT XXII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N F n it XXII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXII-5-5 Ph H H CH ₂ Ph CH ₃ N F n it XXII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n F n it XXII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXII-5-8 Ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-6-1 p-me-ph H H H CH ₃ N F N IT XXII-6-2 p-me-ph H H CH ₃ CH ₃ N F N IT XXII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N F N IT XXII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT XXII-6-5 p-me-ph H H CH ₂ Ph CH ₃ N F N IT XXII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N F N IT XXII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT XXII-6-8 p-me-ph * H * CH ₃ N F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-7-1 p-f-ph H H H CH ₃ n F N IT XXII-7-2 p-f-ph H H CH ₃ CH ₃ n F N IT XXII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n F N IT XXII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT XXII-7-6 p-f-ph H H CH ₂ Ph CH ₃ n F N IT XXII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n F N IT XXII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT XXII-7-20 p-f-ph * H * CH ₃ n F N it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-8-1 p-Cl-Ph H H H CH ₃ N F N IT XXII-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F N IT XXII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n F N IT XXII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT XXII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n F N IT XXII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n F N IT XXII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F N it XXII-8-8 p-Cl-Ph * H * CH ₃ n F N it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-9-1 p-Br-Ph H H H CH ₃ N F n IT XXII-9-2 p-Br-Ph H H CH ₃ CH ₃ N F n it XXII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F n it XXII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F n it XXII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N F n it XXII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXII-9-20 p-Br-Ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-10-1 p-1-ph N n n CH ₃ N F N IT XXII-10-2 p-1-ph N n CH ₃ CH ₃ N F N IT XXII-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ N F n IT XXII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXII-10-5 p-1-ph n n CH ₂ Ph CH ₃ N F n it XXII-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N F n it XXII-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ N F n it XXII-10-8 p-1-ph n CH ₃ N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-11-1 CH ₃ N N n Et H F H OH XXII-11-2 CH ₃ n N CH ₃ Et H F H OH XXII-11-Z CH ₃ N N CH (CH ₃ ) ₂ Et H F H OH XXII-11-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-11-5 CH ₃ n n CH ₂ Ph Et H F H OH XXII-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H F H OH XXII-11-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-11-8 CH ₃ * n * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-12-1 Et H H H Et H F H OH XXII-12-2 Et H H CH ₃ Et H F H OH XXII-12-3 Et H H CH (CH ₃ ) ₂ Et H F H OH XXII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-12-5 Et H H CH ₂ Ph Et H F H OH XXII-12-6 Et H H CH ₂ -indol-3-yl Et H F H OH XXII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-12-8 Et * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-13-1 ⁱ Pr N N n Et H F H OH XXII-13-2 ⁱ Pr N N CH ₃ Et H F H OH XXII-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H F H OH XXII-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-13-5 ⁱ Pr N n CH ₂ Ph Et H F H OH XXII-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H F H OH XXII-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-13-8 ⁱ Pr n * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-14-1 ^t Bu N N N Et H F H OH XXII-14-2 ^t Bu N N CH ₃ Et H F H OH XXII-14-3 ^t Bu N N CH (CH ₃ ) ₂ Et H F H OH XXII-14-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-14-5 ^t Bu N n CH ₂ Ph Et H F H OH XXII-14-6 ^t Bu N n CH ₂ -indol-3-yl Et H F H OH XXII-14-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-14-8 ^t Bu * n * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-15-1 Ph H H H Et H F H OH XXII-15-2 Ph H H CH ₃ Et H F H OH XXII-15-3 Ph H H CH (CH ₃ ) ₂ Et H F H OH XXII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-15-5 Ph H H CH ₂ Ph Et H F H OH XXII-15-6 Ph H H CH ₂ -indol-3-yl Et H F H OH XXII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-15-8 Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-16-1 p-me-ph H H H Et H F H OH XXII-16-2 p-me-ph H H CH ₃ Et H F H OH XXII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F H OH XXII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-16-5 p-me-ph H H CH ₂ Ph Et H F H OH XXII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F H OH XXII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXIH6-8 p-me-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-17-1 p-f-ph H H H Et H F H OH XXII-17-2 p-f-ph H H CH ₃ Et H F H OH XXII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F H OH XXII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-17-5 p-f-ph H H CH ₂ Ph Et H F H OH XXII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F H OH XXII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-17-8 p-f-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIM8-1 p-Cl-Ph H H H Et H F H OH XXII-18-2 p-Cl-Ph H H CH ₃ Et H F H OH XXII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F H OH XXII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-18-5 p-Cl-Ph H H CH ₂ Ph Et H F H OH XXII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F H OH XXII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-18-8 p-Cl-Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-19-1 p-Br-Ph H H H Et H F H OH XXII-19-2 p-Br-Ph H H CH ₃ Et H F H OH XXII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F H OH XXII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-19-5 p-Br-Ph H H CH ₂ Ph Et H F H OH XXII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F H OH XXII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-19-8 p-Br-Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-20-1 p-1-ph N N n Et H F H OH XXII-20-2 p-1-ph N N CH ₃ Et H F H OH XXII-20-3 p-1-ph N N CH (CH ₃ ) ₂ Et H F H OH XXII-20-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXII-20-5 p-1-ph N N CH ₂ Ph Et H F H OH XXII-20-6 p-1-ph N N CH ₂ -indol-3-yl Et H F H OH XXII-20-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ Et H F H OH XXII-20-8 p-1-ph * N * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-21-1 CH ₃ N N n ⁱ Pr N F n IT XXII-21-2 CH ₃ N N CH ₃ ⁱ Pr N F n IT XXII-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr n F n IT XXII-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F n it XXII-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr n F n it XXII-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr n F n it XXII-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it XXII-21-8 CH ₃ * n * ⁱ Pr n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-22-1 Et H H H ⁱ Pr H F H OH XXII-22-2 Et H H CH ₃ ⁱ Pr H F H OH XXII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-22-5 Et H H CH ₂ Ph ⁱ Pr H F H OH XXII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXII-22-8 Et * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-23-1 ⁱ Pr N n n ⁱ Pr N F N IT XXII-23-2 ⁱ Pr N n CH ₃ ⁱ Pr N F n IT XXII-23-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁱ Pr n F n it XXII-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F n it XXII-23-5 ⁱ Pr n n CH ₂ Ph ⁱ Pr n F n it XXII-23-6 ⁱ Pr n n CH ₂ -indol-3-yl ⁱ Pr n F n it XXII-23-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it XXII-23-8 ⁱ Pr * n * ⁱ Pr n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-24-1 ^t Bu N n n ⁱ Pr N F N IT XXII-24-2 ^t Bu n n CH ₃ ⁱ Pr N F N IT XXII-24-3 ^t Bu N n CH (CH ₃ ) ₂ ⁱ Pr N F n IT XXII-24-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F n it XXII-24-5 ^t Bu n n CH ₂ Ph ⁱ Pr N F n it XXII-24-6 ^t Bu n n CH ₂ -indol-3-yl ⁱ Pr N F n it XXII-24-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F n it XXII-24-8 ^t Bu * n * ⁱ Pr N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-25-1 Ph H H H ⁱ Pr H F H OH XXII-25-2 Ph H H CH ₃ ⁱ Pr H F H OH XXII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-25-5 Ph H H CH ₂ Ph ⁱ Pr H F H OH XXII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXII-2S-8 Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-26-1 p-me-ph H H H ⁱ Pr H F H OH XXII-26-2 p-me-ph H H CH ₃ ⁱ Pr H F H OH XXII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F H OH XXII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXII-26-8 p-me-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-27-1 p-f-ph H H H ⁱ Pr H F H OH XXII-27-2 p-f-ph H H CH ₃ ⁱ Pr H F H OH XXII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F H OH XXII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXII-27-8 p-f-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-28-1 p-Cl-Ph H H H ⁱ Pr H F H OH XXII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F H OH XXII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F H OH XXII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXII-28-8 p-Cl-Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-29-1 p-Br-Ph H H H ⁱ Pr H F H OH XXII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F H OH XXII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F H OH XXII-29-b p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXII-29-8 p-Br-Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-30-1 p-1-ph N N n ⁱ Pr N F n IT XXII-30-2 p-1-ph N n CH ₃ ⁱ Pr N F n IT XXII-30-3 p-1-ph N n CH (CH ₃ ) ₂ ⁱ Pr n F n it XXII-30-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F n it XXII-30-5 p-1-ph N n CH ₂ Ph ⁱ Pr n F n it XXII-30-6 p-1-ph N n CH ₂ -indol-3-yl ⁱ Pr n F n it XXII-30-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it XXII-30-8 p-1-ph * n * ⁱ Pr n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-31-1 CH ₃ N N N ⁿ Bu H F H OH XXII-31-2 CH ₃ N N CH ₃ ⁿ Bu H F H OH XXII-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H F H OH XXII-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-31-8 CH ₃ * n * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-32-1 Et H H H ⁿ Bu H F H OH XXII-32-2 Et H H CH ₃ ⁿ Bu H F H OH XXII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-32-5 Et H H CH ₂ Ph ⁿ Bu H F H OH XXII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-32-8 Et * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-33-1 ⁱ Pr N N N ⁿ Bu H F H OH XXII-33-2 ⁱ Pr N N CH ₃ ⁿ Bu H F H OH XXII-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-33-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-33-5 ⁱ Pr N N CH ₂ Ph ⁿ Bu H F H OH XXII-33-6 ⁱ Pr N N CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-33-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-33-8 ⁱ Pr * N * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-34-1 ⁿ Bu N n n ⁿ Bu H F H OH XXII-34-2 ⁿ Bu N n CH ₃ ⁿ Bu H F H OH XXII-34-3 ⁿ Bu N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-34-4 ⁿ Bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-34-5 ⁿ Bu N n CH ₂ Ph ⁿ Bu H F H OH XXII-34-6 ⁿ Bu N n CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-34-7 ⁿ Bu n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-34-8 ⁿ Bu * n * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-35-1 Ph H H H ⁿ Bu H F H OH XXII-35-2 Ph H H CH ₃ ⁿ Bu H F H OH XXII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-35-5 Ph H H CH ₂ Ph ⁿ Bu H F H OH XXII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-35-8 Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-36-1 p-me-ph H H H ⁿ Bu H F H OH XXII-36-2 p-me-ph H H CH ₃ ⁿ Bu H F H OH XXII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F H OH XXII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-36-8 p-me-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-37-1 p-f-ph H H H ⁿ Bu H F H OH XXII-37-2 p-f-ph H H CH ₃ ⁿ Bu H F H OH XXII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F H OH XXII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-37-8 p-f-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-38-1 p-Cl-Ph H H H ⁿ Bu H F H OH XXII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F H OH XXII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F H OH XXII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-38-8 p-Cl-Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-39-1 p-Br-Ph H H H ⁿ Bu H F H OH XXII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F H OH XXII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F H OH XXII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-39-8 p-Br-Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-40-1 p-1-ph N n n ⁿ Bu H F H OH XXII-40-2 p-1-ph N n CH ₃ . ⁿ Bu H F H OH XXII-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXII-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H F H OH XXII-40-6 p-1-ph n n CH ₂ -indol-3-yl ⁿ Bu H F H OH XXII-40-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXII-40-8 p-1-ph * n * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-41-1 CH ₃ N N N Bz H F H OH XXII-41-2 CH ₃ N N CH ₃ Bz H F H OH XXII-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H F H OH XXII-41-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-41-5 CH ₃ N N CH ₂ Ph Bz H F H OH XXII-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H F H OH XXII-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-41-8 CH ₃ * n * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-42-1 Et H H H Bz H F H OH XXII-42-2 Et H H CH ₃ Bz H F H OH XXII-42-3 Et H H CH (CH ₃ ) ₂ Bz H F H OH XXII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-42-5 Et H H CH ₂ Ph Bz H F H OH XXII-42-6 Et H H CH ₂ -indol-3-yl Bz H F H OH XXII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-42-8 Et * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-43-1 ⁱ Pr H H N Bz H F H OH XXII-43-2 ⁱ Pr H H CH ₃ Bz H F H OH XXII-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H F H OH XXII-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH HHP-43-5 ⁱ Pr H H CH ₂ Ph Bz H F H OH HHP-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H F H OH HHP-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXN-43-8 ⁱ Pr * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-44-1 ^t Bu N N n Bz H F H OH XXII-44-2 ^t Bu N n CH ₃ Bz H F H OH XXII-44-3 ^t Bu N N CH (CH ₃ ) ₂ Bz H F H OH XXII-44-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-44-5 ^t Bu N N CH ₂ Ph Bz H F H OH XXII-44-6 ^t Bu N N CH ₂ -indol-3-yl Bz H F H OH XXII-44-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-44-8 ^t Bu * n * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-45-1 Ph H H H Bz H F H OH XXII-45-2 Ph H H CH ₃ Bz H F H OH XXII-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-45-5 Ph H H CH ₂ Ph Bz H F H OH XXII-45-6 Ph H H CH ₂ -indol-3-yl Bz H F H OH XXII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-45-8 Ph * H Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-46-1 p-me-ph H H H Bz H F H OH XXII-46-2 p-me-ph H H CH ₃ Bz H F H OH XXII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-46-5 p-me-ph H H CH ₂ Ph Bz H F H OH XXII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F H OH XXII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-46-8 p-me-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-47-1 p-f-ph H H H Bz H F H OH XXII-47-2 p-f-ph H H CH ₃ Bz H F H OH XXII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-47-5 p-f-ph H H CH ₂ Ph Bz H F H OH XXII-47-b p-f-ph H H CH ₂ -indol-3-yl Bz H F H OH XXII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-47-8 p-f-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-48-1 p-Cl-Ph H H H Bz H F H OH XXII-48-2 p-Cl-Ph H H CH ₃ Bz H F H OH XXII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F H OH XXII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F H OH; XXII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-48-8 p-Cl-Ph H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-49-1 p-Br-Ph H H H Bz H F H OH XXII-49-2 p-Br-Ph H H CH ₃ Bz H F H OH XXII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-49-5 p-Br-Ph H H CH ₂ Ph Bz H F H OH XXII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F H OH XXII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-49-8 p-Br-Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXII-50-1 p-1-ph N N n Bz H F H OH XXII-50-2 p-1-ph N N CH ₃ Bz H F H OH XXII-50-3 p-1-ph N N CH (CH ₃ ) ₂ Bz H F H OH XXII-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXII-50-5 p-1-ph N n CH ₂ Ph Bz H F H OH XXII-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H F H OH XXII-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H F H OH XXII-50-8 p-1-ph * n * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-1-1 CH ₃ N N n CH ₃ N F F IT XXIII-1-2 CH ₃ N N CH ₃ CH ₃ N F F IT XXIII-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N F F IT XXIII-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT XXIII-1-5 CH ₃ N n CH ₂ Ph CH ₃ N F F IT XXIII-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N F F IT XXIII-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT XXIII-1-8 CH ₃ * n * CH ₃ N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-2-1 Et H H H CH ₃ N F F IT XXIII-2-2 Et H H CH ₃ CH ₃ N F F IT XXIII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N F F it XXIII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F it XXIII-2-5 Et H H CH ₂ Ph CH ₃ N F F it XXIII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N F F it XXIII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F it XXIII-2-8 Et * H * CH ₃ N F F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-3-1 ⁱ Pr N n n CH ₃ N F F IT XXIII-3-2 ⁱ Pr N n CH ₃ CH ₃ n F F IT XXIII-3-3 ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ n F F IT XXIII-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT XXIII-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ n F F IT XXIII-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ n F F IT XXIII-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXIII-3-8 ⁱ Pr * n * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-4-1 ^t Bu N N n CH ₃ N F F IT XXIII-4-2 ^t Bu N N CH ₃ CH ₃ N F F IT XXIII-4-3 ^t Bu N n CH (CH ₃ ) ₂ CH ₃ N F F IT XXIII-4-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT XXIII-4-5 ^t Bu N n CH ₂ Ph CH ₃ N F F IT XXIII-4-6 ^t Bu N n CH ₂ -indol-3-yl CH ₃ N F F IT XXIII-4-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT XXIII-4-8 ^t Bu * n * CH ₃ N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-5-1 Ph H H H CH ₃ H F F OH XXIII-5-2 Ph H H CH ₃ CH ₃ H F F OH XXIII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXIII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXIII-5-5 Ph H H CH ₂ Ph CH ₃ H F F OH XXIII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ H F F OH XXIII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXIII-5-8 Ph * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-6-1 p-me-ph H H H CH ₃ H F F OH XXIII-6-2 p-me-ph H H CH ₃ CH ₃ H F F OH XXIII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXIII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXIII-6-5 p-me-ph H H CH ₂ Ph CH ₃ H F F OH XXIII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ H F F OH XXIII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXIII-6-8 p-me-ph * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-7-1 p-f-ph H H H CH ₃ H F F OH XXIII-7-2 p-f-ph H H CH ₃ CH ₃ H F F OH XXIII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXIII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXIII-7-6 p-f-ph H H CH ₂ Ph CH ₃ H F F OH XXIII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ H F F OH XXIII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXIII-7-20 p-f-ph * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-8-1 p-Cl-Ph H H H CH ₃ N F F IT XXIII-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F F IT XXIII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT XXIII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT XXIII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n F F IT XXIII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n F F IT XXIII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXIII-8-8 p-Cl-Ph * H * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-9-1 p-Br-Ph H H H CH ₃ N F F IT XXIII-9-2 p-Br-Ph H H CH ₃ CH ₃ N F F IT XXIII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT XXIII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT XXIII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n F F IT XXIII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n F F IT XXIII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXIII-9-20 p-Br-Ph * H * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-10-1 p-1-ph N N N CH ₃ N F F IT XXIII-10-2 p-1-ph N N CH ₃ CH ₃ N F F IT XXIII-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N F F it XXIII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F it XXIII-10-5 p-1-ph N n CH ₂ Ph CH ₃ N F F it XXIII-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ N F F it XXIII-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ N F F it XXIII-10-8 p-1-ph * n * CH ₃ N F F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-11-1 CH ₃ N N N Et H F F OH XXIII-11-2 CH ₃ N N CH ₃ Et H F F OH XXIII-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H F F OH XXIII-11-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-11-5 CH ₃ N N CH ₂ Ph Et H F F OH XXIII-11-6 CH ₃ N N CH ₂ -indol-3-yl Et H F F OH XXIII-11-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-11-8 CH ₃ * N * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-12-1 Et H H H Et H F F OH XXIII-12-2 Et H H CH ₃ Et H F F OH XXIII-12-3 Et H H CH (CH ₃ ) ₂ Et H F F OH XXIII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-12-5 Et H H CH ₂ Ph Et H F F OH XXIII-12-6 Et H H CH ₂ -indol-3-yl Et H F F OH XXIII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-12-8 Et * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-13-1 ⁱ Pr N n n Et H F F OH XXIII-13-2 ⁱ Pr N n CH ₃ Et H F F OH XXIII-13-3 ⁱ Pr n n CH (CH ₃ ) ₂ Et H F F OH XXIII-13-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-13-5 ⁱ Pr n n CH ₂ Ph Et H F F OH XXIII-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et H F F OH XXIII-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-13-8 ⁱ Pr * n * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-14-1 ^t Bu N n n Et H F F OH XXIII-14-2 ^t Bu N n CH ₃ Et H F F OH XXIII-14-3 ^t Bu N n CH (CH ₃ ) ₂ Et H F F OH XXIII-14-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-14-5 ^t Bu n n CH ₂ Ph Et H F F OH XXIII-14-6 ^t Bu n n CH ₂ -indol-3-yl Et H F F OH XXIII-14-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-14-8 ^t Bu * n * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-15-1 Ph H H H Et H F F OH XXIII-15-2 Ph H H CH ₃ Et H F F OH XXIII-15-3 Ph H H CH (CH ₃ ) ₂ Et H F F OH XXIII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-15-5 Ph H H CH ₂ Ph Et H F F OH XXIII-15-6 Ph H H CH ₂ -indol-3-yl Et H F F OH XXIII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-15-8 Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-16-1 p-me-ph H H H Et H F F OH XXIII-16-2 p-me-ph H H CH ₃ Et H F F OH XXIII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F F OH XXIII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-16-5 p-me-ph H H CH ₂ Ph Et H F F OH XXIII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F F OH XXIII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-16-8 p-me-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-17-1 p-f-ph H H H Et H F F OH XXIII-17-2 p-f-ph H H CH ₃ Et H F F OH XXIII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F F OH XXIII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-17-5 p-f-ph H H CH ₂ Ph Et H F F OH XXIII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F F OH XXIII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-17-8 p-f-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-18-1 p-Cl-Ph H H H Et H F F OH XXIII-18-2 p-Cl-Ph H H CH ₃ Et H F F OH XXIII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F F OH XXIII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-18-5 p-Cl-Ph H H CH ₂ Ph Et H F F OH XXIII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F F OH XXIII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-18-8 p-Cl-Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-19-1 p-Br-Ph H H H Et H F F OH XXIII-19-2 p-Br-Ph H H CH ₃ Et H F F OH XXIII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F F OH XXIII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-19-5 p-Br-Ph H H CH ₂ Ph Et H F F OH XXIII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F F OH XXIII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-19-8 p-Br-Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-20-1 p-1-ph N n n Et H F F OH XXIII-20-2 p-1-ph N n CH ₃ Et H F F OH XXIII-20-3 p-1-ph N n CH (CH ₃ ) ₂ Et H F F OH XXIII-20-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXIII-20-5 p-1-ph N n CH ₂ Ph Et H F F OH XXIII-20-6 p-1-ph N n CH ₂ -indol-3-yl Et H F F OH XXIII-20-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Et H F F OH XXIII-20-8 p-1-ph * n * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-21-1 CH ₃ N N n ⁱ Pr N F F IT XXIII-21-2 CH ₃ N N CH ₃ ⁱ Pr N F F IT XXIII-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N F F IT XXIII-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT XXIII-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr N F F IT XXIII-21-6 CH ₃ N N CH ₂ -indol-3-yl ⁱ Pr N F F IT XXIII-21-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT XXIII-21-8 CH ₃ * N * ⁱ Pr N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-22-1 Et H H H ⁱ Pr H F F OH XXIII-22-2 Et H H CH ₃ ⁱ Pr H F F OH XXIII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-22-5 Et H H CH ₂ Ph ⁱ Pr H F F OH XXIII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXIII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXIII-22-8 Et * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-23-1 ⁱ Pr N N n ⁱ Pr N F F IT XXIII-23-2 ⁱ Pr N N CH ₃ ⁱ Pr N F F IT XXIII-23-3 ⁱ Pr N n CH (CH ₃ ) ₂ ⁱ Pr n F F IT XXIII-23-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F F IT XXIII-23-5 ⁱ Pr N n CH ₂ Ph ⁱ Pr n F F IT XXIII-23-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁱ Pr n F F IT XXIII-23-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F F IT XXIII-23-8 ⁱ Pr * n * ⁱ Pr n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-24-1 ^t Bu N n n ⁱ Pr N F F IT XXIII-24-2 ^t Bu N n CH ₃ ⁱ Pr N F F IT XXIH-24-3 ^t Bu N n CH (CH ₃ ) ₂ ⁱ Pr N F F IT XXIII-24-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT XXIII-24-5 ^t Bu N n CH ₂ Ph ⁱ Pr N F F IT XXIII-24-6 ^t Bu N n CH ₂ -indol-3-yl ⁱ Pr N F F IT XXIII-24-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT XXIII-24-8 ^t Bu * n * ⁱ Pr N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-25-1 Ph H H H ⁱ Pr H F F OH XXIII-25-2 Ph H H CH ₃ ⁱ Pr H F F OH XXIII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-25-5 Ph H H CH ₂ Ph ⁱ Pr H F F OH XXIII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXIII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXIII-25-8 Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-26-1 p-me-ph H H H ⁱ Pr H F F OH XXIII-26-2 p-me-ph H H CH ₃ ⁱ Pr H F F OH XXIII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F F OH XXIII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXIII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXIII-26-8 p-me-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-27-1 p-f-ph H H H ⁱ Pr H F F OH XXIII-27-2 p-f-ph H H CH ₃ ⁱ Pr H F F OH XXIII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F F OH XXIII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXIII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXIII-27-8 p-f-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-28-1 p-Cl-Ph H H H ⁱ Pr H F F OH XXIII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F F OH XXIII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F F OH XXIII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXIII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXIII-28-8 p-Cl-Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-29-1 p-Br-Ph H H H ⁱ Pr H F F OH XXIII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F F OH XXIII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXIII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F F OH XXIII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXIII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXIII-29-8 p-Br-Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-30-1 p-1-ph N N n ⁱ Pr N F F IT XXIII-30-2 p-1-ph N N CH ₃ ⁱ Pr N F F IT XXIII-30-3 p-1-ph N N CH (CH ₃ ) ₂ ⁱ Pr N F F IT XXIII-30-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F IT XXIII-30-5 p-1-ph N N CH ₂ Ph ⁱ Pr N F F IT XXIII-30-6 p-1-ph N N CH ₂ -indol-3-yl ⁱ Pr N F F IT XXIII-30-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F IT XXIII-30-8 p-1-ph * n * ⁱ Pr N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-31-1 CH ₃ N N n ⁿ Bu H F F OH XXIII-31-2 CH ₃ N n CH ₃ ⁿ Bu H F F OH XXIII-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H F F OH XXIII-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-31-8 CH ₃ * n * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-32-1 Et H H H ⁿ Bu H F F OH XXIII-32-2 Et H H CH ₃ ⁿ Bu H F F OH XXIII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-32-5 Et H H CH ₂ Ph ⁿ Bu H F F OH XXIII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-32-8 Et * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-33-1 ⁱ Pr H H H ⁿ Bu H F F OH XXIII-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H F F OH XXIII-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H F F OH XXIII-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-33-8 ⁱ Pr H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-34-1 ^t Bu H H H ⁿ Bu H F F OH XXIII-34-2 ^t Bu H H CH ₃ ⁿ Bu H F F OH XXIII-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H F F OH XXIII-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-34-8 ^t Bu * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-35-1 Ph H H H ⁿ Bu H F F OH XXIII-35-2 Ph H H CH ₃ ⁿ Bu H F F OH XXIII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-35-5 Ph H H CH ₂ Ph ⁿ Bu H F F OH XXIII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-35-8 Ph H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-36-1 p-me-ph H H H ⁿ Bu H F F OH XXIII-36-2 p-me-ph H H CH ₃ ⁿ Bu H F F OH XXIII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F F OH XXIII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-36-8 p-me-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-37-1 p-f-ph H H H ⁿ Bu H F F OH XXIII-37-2 p-f-ph H H CH ₃ ⁿ Bu H F F OH XXIII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F F OH XXIII-37-b p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-37-8 p-f-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-38-1 p-Cl-Ph H H H ⁿ Bu H F F OH XXIII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F F OH XXIII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F F OH XXIII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-38-8 p-Cl-Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-39-1 p-Br-Ph H H H ⁿ Bu H F F OH XXIII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F F OH XXIII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F F OH XXIII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-39-8 p-Br-Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-40-1 p-i-ph H H H ⁿ Bu H F F OH XXIII-40-2 p-i-ph H H CH ₃ ⁿ Bu H F F OH XXIII-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXIII-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H F F OH XXIII-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXIII-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXIII-40-8 p-i-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-41-1 CH ₃ N N N Bz H F F OH XXIII-41-2 CH ₃ N N CH ₃ Bz H F F OH XXIII-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H F F OH XXIII-41-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-41-5 CH ₃ N N CH ₂ Ph Bz H F F OH XXIII-41-6 CH ₃ N N CH ₂ -indol-3-yl Bz H F F OH XXIII-41-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-41-8 CH ₃ * N * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-42-1 Et H H H Bz H F F OH XXIII-42-2 Et H H CH ₃ Bz H F F OH XXIII-42-3 Et H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-42-5 Et H H CH ₂ Ph Bz H F F OH XXIII-42-6 Et H H CH ₂ -indol-3-yl Bz H F F OH XXIII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-42-8 Et * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-43-1 ⁱ Pr H H H Bz H F F OH XXIII-43-2 ⁱ Pr H H CH ₃ Bz H F F OH XXIII-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-43-5 ⁱ Pr H H CH ₂ Ph Bz H F F OH XXIII-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H F F OH XXIII-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-43-8 ⁱ Pr * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-44-1 ^t Bu H H H Bz H F F OH XXIII-44-2 ^t Bu H H CH ₃ Bz H F F OH XXIII-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-44-5 ^t Bu H H CH ₂ Ph Bz H F F OH XXIII-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H F F OH XXIII-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-44-8 ^t Bu * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-45-1 Ph H H H Bz H F F OH XXIII-45-2 Ph H H CH ₃ Bz H F F OH XXIII-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-45-5 Ph H H CH ₂ Ph Bz H F F OH XXIII-45-6 Ph H H CH ₂ -indol-3-yl Bz H F F OH XXIII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-45-8 Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-46-1 p-me-ph H H H Bz H F F OH XXIII-46-2 p-me-ph H H CH ₃ Bz H F F OH XXIII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-46-5 p-me-ph H H CH ₂ Ph Bz H F F OH XXIII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F F OH XXIII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-46-8 p-me-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-47-1 p-f-ph H H H Bz H F F OH XXIII-47-2 p-f-ph H H CH ₃ Bz H F F OH XXIII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-47-5 p-f-ph H H CH ₂ Ph Bz H F F OH XXIII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F F OH XXIII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-47-8 p-f-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-48-1 p-Cl-Ph H H H Bz H F F OH XXIII-48-2 p-Cl-Ph H H CH ₃ Bz H F F OH XXIII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F F OH XXIII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F F OH XXIII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-48-8 p-Cl-Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-49-1 p-Br-Ph H H H Bz H F F OH XXIII-49-2 p-Br-Ph H H CH ₃ Bz H F F OH XXIII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-49-5 p-Br-Ph H H CH ₂ Ph Bz H F F OH XXIII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F F OH XXIII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-49-8 p-Br-Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIII-50-1 p-i-ph H H H Bz H F F OH XXIII-50-2 p-i-ph H H CH ₃ Bz H F F OH XXIII-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXIII-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXIII-50-5 p-i-ph H H CH ₂ Ph Bz H F F OH XXIII-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H F F OH XXIII-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXIII-50-8 p-i-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-1-1 CH ₃ N N n CH ₃ N N F IT XXIV-1-2 CH ₃ N N CH ₃ CH ₃ N N F IT XXIV-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N N F IT XXIV-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXIV-1-5 CH ₃ N n CH ₂ Ph CH ₃ N N F IT XXIV-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ n n F IT XXIV-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXIV-1-8 CH ₃ * n * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-2-1 Et H H H CH ₃ N N F IT XXIV-2-2 Et H H CH ₃ CH ₃ N N F IT XXIV-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ n N F IT XXIV-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n N F IT XXIV-2-5 Et H H CH ₂ Ph CH ₃ n n F IT XXIV-2-6 Et H H CH ₂ -indol-3-yl CH ₃ n n F IT XXIV-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXIV-2-8 Et * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-3-1 ⁱ Pr N N N CH ₃ N N F it XXIV-3-2 ⁱ Pr N N CH ₃ CH ₃ n N F it XXIV-3-3 ⁱ Pr N N CH (CH ₃ ) ₂ CH ₃ n N F IT XXIV-3-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT XXIV-3-5 ⁱ Pr N N CH ₂ Ph CH ₃ n n F IT XXIV-3-6 ⁱ Pr N N CH ₂ -indol-3-yl CH ₃ n n F IT XXIV-3-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXIV-3-8 ⁱ Pr * N * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-4-1 ^t bu N n n CH ₃ N N F IT XXIV-4-2 ^t bu N n CH ₃ CH ₃ N N F IT XXIV-4-3 ^t bu n n CH (CH ₃ ) ₂ CH ₃ N N F IT XXIV-4-4 ^t bu N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXIV-4-5 ^t bu N n CH ₂ Ph CH ₃ N N F IT XXIV-4-6 ^t bu N n CH ₂ -indol-3-yl CH ₃ N N F IT XXIV-4-7 ^t bu N n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT XXIV-4-8 ^t bu * n * CH ₃ N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-5-1 Ph H H H CH ₃ n n f it XXIV-5-2 Ph H H CH ₃ CH ₃ n n f it XXIV-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n n f it XXIV-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n f it XXIV-5-5 Ph H H CH ₂ Ph CH ₃ n n f it XXIV-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n n f it XXIV-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n f it XXIV-5-8 Ph * H * CH ₃ n n f it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-6-1 p-me-ph H H H CH ₃ N N F IT XXIV-6-2 p-me-ph H H CH ₃ CH ₃ N N F IT XXIV-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT XXIV-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n N F IT XXIV-6-5 p-me-ph H H CH ₂ Ph CH ₃ n n F IT XXIV-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n n F IT XXIV-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXIV-6-8 p-me-ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-7-1 p-f-ph H H H CH ₃ N N F IT XXIV-7-2 p-f-ph H H CH ₃ CH ₃ N N F IT XXIV-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N n F IT XXIV-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT XXIV-7-6 p-f-ph H H CH ₂ Ph CH ₃ N n F IT XXIV-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N n F IT XXIV-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT XXIV-7-20 p-f-ph * H * CH ₃ N n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-8-1 p-Cl-Ph H H H CH ₃ N n F IT XXIV-8-2 p-Cl-Ph H H CH ₃ CH ₃ N n F IT XXIV-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n n F IT XXIV-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT XXIV-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n n F IT XXIV-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n n F IT XXIV-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXIV-8-8 p-Cl-Ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-9-1 p-Br-Ph H H H CH ₃ N n F IT XXIV-9-2 p-Br-Ph H H CH ₃ CH ₃ N n F IT XXIV-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N n F IT XXIV-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT XXIV-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N n F IT XXIV-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n n F IT XXIV-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXIV-9-20 p-Br-Ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-10-1 p-i-ph H H H CH ₃ N N F IT XXIV-10-2 p-i-ph H H CH ₃ CH ₃ N N F IT XXIV-10-3 p-i-ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT XXIV-10-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT XXIV-10-5 p-i-ph H H CH ₂ Ph CH ₃ N n F IT XXIV-10-6 p-i-ph H H CH ₂ -indol-3-yl CH ₃ N n F IT XXIV-10-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT XXIV-10-8 p-i-ph * H * CH ₃ N n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-11-1 CH ₃ N N n Et H H F OH XXIV-11-2 CH ₃ N n CH ₃ Et H H F OH XXIV-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H H F OH XXIV-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-11-5 CH ₃ N n CH ₂ Ph Et H H F OH XXIV-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H H F OH XXIV-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-11-8 CH ₃ n * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-12-1 Et H H H Et H H F OH XXIV-12-2 Et H H CH ₃ Et H H F OH XXIV-12-3 Et H H CH (CH ₃ ) ₂ Et H H F OH XXIV-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-12-5 Et H H CH ₂ Ph Et H H F OH XXIV-12-6 Et H H CH ₂ -indol-3-yl Et H H F OH XXIV-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-12-8 Et * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-13-1 ⁱ Pr H H H Et H H F OH XXIV-13-2 ⁱ Pr H H CH ₃ Et H H F OH XXIV-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et H H F OH XXIV-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-13-5 ⁱ Pr H H CH ₂ Ph Et H H F OH XXIV-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et H H F OH XXIV-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-13-8 ⁱ Pr * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-14-1 ^t Bu H H H Et H H F OH XXIV-14-2 ^t Bu H H CH ₃ Et H H F OH XXIV-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H H F OH XXIV-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-14-5 ^t Bu H H CH ₂ Ph Et H H F OH XXIV-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H H F OH XXIV-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-14-8 ^t Bu * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-15-1 Ph H H H Et H H F OH XXIV-15-2 Ph H H CH ₃ Et H H F OH XXIV-15-3 Ph H H CH (CH ₃ ) ₂ Et H H F OH XXIV-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-15-5 Ph H H CH ₂ Ph Et H H F OH XXIV-15-6 Ph H H CH ₂ -indol-3-yl Et H H F OH XXIV-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-15-8 Ph H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-16-1 p-me-ph H H H Et H H F OH XXIV-16-2 p-me-ph H H CH ₃ Et H H F OH XXIV-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H H F OH XXIV-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-16-5 p-me-ph H H CH ₂ Ph Et H H F OH XXIV-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H H F OH XXIV-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-16-8 p-me-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-17-1 p-f-ph H H H Et H H F OH XXIV-17-2 p-f-ph H H CH ₃ Et H H F OH XXIV-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H H F OH XXIV-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-17-5 p-f-ph H H CH ₂ Ph Et H H F OH XXIV-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H H F OH XXIV-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-17-8 p-f-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-18-1 p-Cl-Ph H H H Et H H F OH XXIV-18-2 p-Cl-Ph H H CH ₃ Et H H F OH XXIV-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H H F OH XXIV-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-18-5 p-Cl-Ph H H CH ₂ Ph Et H H F OH XXIV-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H H F OH XXIV-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-18-8 p-Cl-Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-19-1 p-Br-Ph H H H Et H H F OH XXIV-19-2 p-Br-Ph H H CH ₃ Et H H F OH XXIV-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H H F OH XXIV-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-19-5 p-Br-Ph H H CH ₂ Ph Et H H F OH XXIV-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H H F OH XXIV-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-19-8 p-Br-Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-20-1 p-i-ph H H H Et H H F OH XXIV-20-2 p-i-ph H H CH ₃ Et H H F OH XXIV-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H H F OH XXIV-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXIV-20-5 p-i-ph H H CH ₂ Ph Et H H F OH XXIV-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H H F OH XXIV-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXIV-20-8 p-i-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-21-1 CH ₃ N N n ⁱ Pr N N F IT XXIV-21-2 CH ₃ N n CH ₃ ⁱ Pr N N F IT XXIV-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr N N F IT XXIV-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N N F IT XXIV-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N N F IT XXIV-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N N F IT XXIV-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N N F IT XXIV-21-8 CH ₃ * n * ⁱ Pr N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-22-1 Et H H H ⁱ Pr H H F OH XXIV-22-2 Et H H CH ₃ ⁱ Pr H H F OH XXIV-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-22-5 Et H H CH ₂ Ph ⁱ Pr H H F OH XXIV-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-22-8 Et * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-23-1 ⁱ Pr H H H ⁱ Pr H H F OH XXIV-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H H F OH XXIV-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H H F OH XXIV-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-23-8 ⁱ Pr * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-24-1 ^t Bu H H H ⁱ Pr H H F OH XXIV-24-2 ^t Bu H H CH ₃ ⁱ Pr H H F OH XXIV-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H H F OH XXIV-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-24-8 ^t Bu H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-25-1 Ph H H H ⁱ Pr H H F OH XXIV-25-2 Ph H H CH ₃ ⁱ Pr H H F OH XXIV-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ . ⁱ Pr H H F OH XXIV-25-5 Ph H H CH ₂ Ph ⁱ Pr H H F OH XXIV-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-25-8 Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-26-1 p-me-ph H H H ⁱ Pr H H F OH XXIV-26-2 p-me-ph H H CH ₃ ⁱ Pr H H F OH XXIV-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H H F OH XXIV-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-26-8 p-me-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-27-1 p-f-ph H H H ⁱ Pr H H F OH XXIV-27-2 p-f-ph H H CH ₃ ⁱ Pr H H F OH XXIV-27-3 p-f-ph H H CH (CH ₃ ) ₂ * Pr H H F OH XXIV-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H H F OH XXIV-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-27-8 p-f-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-28-1 p-Cl-Ph H H H ⁱ Pr H H F OH XXIV-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H H F OH XXIV-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H H F OH XXIV-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-28-8 p-Cl-Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-29-1 p-Br-Ph H H H ⁱ Pr H H F OH XXIV-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H H F OH XXIV-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H H F OH XXIV-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-29-8 p-Br-Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-30-1 p-i-ph H H H ⁱ Pr H H F OH XXIV-30-2 p-i-ph H H CH ₃ ⁱ Pr H H F OH XXIV-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXIV-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H H F OH XXIV-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXIV-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXIV-30-8 p-i-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-31-1 CH ₃ N n n ⁿ Bu H H F OH XXIV-31-2 CH ₃ N n CH ₃ ⁿ Bu H H F OH XXIV-31-3 CH ₃ n n CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-31-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-31-5 CH ₃ n n CH ₂ Ph ⁿ Bu H H F OH XXIV-31-6 CH ₃ n n CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-31-8 CH ₃ * n * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-32-1 Et H H H ⁿ Bu H H F OH XXIV-32-2 Et H H CH ₃ ⁿ Bu H H F OH XXIV-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-32-5 Et H H CH ₂ Ph ⁿ Bu H H F OH XXIV-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-32-8 Et * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-33-1 ⁱ Pr H H H ⁿ Bu H H F OH XXIV-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H H F OH XXIV-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H H F OH XXIV-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-33-8 ⁱ Pr * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-34-1 ^t Bu H H H ⁿ Bu H H F OH XXIV-34-2 ^t Bu H H CH ₃ ⁿ Bu H H F OH XXIV-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H H F OH XXIV-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-34-8 ^t Bu * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-35-1 Ph H H H ⁿ Bu H H F OH XXIV-35-2 Ph H H CH ₃ ⁿ Bu H H F OH XXIV-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-35-5 Ph H H CH ₂ Ph ⁿ Bu H H F OH XXIV-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-35-8 Ph * H * ⁿ Bu H H F OH * RZ and RJb are connected to each other via (CH ₂ ) s to form a five-membered ring. Table XXIV-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-36-1 p-me-ph H H H ⁿ Bu H H F OH XXIV-36-2 p-me-ph H H CH ₃ ⁿ Bu H H F OH XXIV-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H H F OH XXIV-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-36-8 p-me-ph H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-37-1 p-f-ph H H H ⁿ Bu H H F OH XXIV-37-2 p-f-ph H H CH ₃ ⁿ Bu H H F OH XXIV-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H H F OH XXIV-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-37-8 p-f-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-38-1 p-Cl-Ph H H H ⁿ Bu H H F OH XXIV-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H H F OH XXIV-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H H F OH XXIV-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-38-8 p-Cl-Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-39-1 p-Br-Ph H H H ⁿ Bu H H F OH XXIV-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H H F OH XXIV-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H H F OH XXIV-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-39-8 p-Br-Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-40-1 p-i-ph H H H ⁿ Bu H H F OH XXIV-40-2 p-i-ph H H CH ₃ ⁿ Bu H H F OH XXIV-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXIV-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H H F OH XXIV-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXIV-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXIV-40-8 p-i-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-41-1 CH ₃ N n n Bz H H F OH XXIV-41-2 CH ₃ N n CH ₃ Bz H H F OH XXIV-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H H F OH XXIV-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-41-5 CH ₃ N n CH ₂ Ph Bz H H F OH XXIV-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H H F OH XXIV-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-41-8 CH ₃ * n * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-42-1 Et H H H Bz H H F OH XXIV-42-2 Et H H CH ₃ Bz H H F OH XXIV-42-3 Et H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-42-5 Et H H CH ₂ Ph Bz H H F OH XXIV-42-6 Et H H CH ₂ -indol-3-yl Bz H H F OH XXIV-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-42-8 Et * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-43-1 ⁱ Pr H H H Bz H H F OH XXIV-43-2 ⁱ Pr H H CH ₃ Bz H H F OH XXIV-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-43-5 ⁱ Pr H H CH ₂ Ph Bz H H F OH XXIV-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H H F OH XXIV-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-43-8 ⁱ Pr * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-44-1 ^t Bu H H H Bz H H F OH XXIV-44-2 ^t Bu H H CH ₃ Bz H H F OH XXIV-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-44-5 ^t Bu H H CH ₂ Ph Bz H H F OH XXIV-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H H F OH XXIV-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-44-8 ^t Bu * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-45-1 Ph H H H Bz H H F OH XXIV-45-2 Ph H H CH ₃ Bz H H F OH XXIV-45-3 Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-45-5 Ph H H CH ₂ Ph Bz H H F OH XXIV-45-6 Ph H H CH ₂ -indol-3-yl Bz H H F OH XXIV-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-45-8 Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-46-1 p-me-ph H H H Bz H H F OH XXIV-46-2 p-me-ph H H CH ₃ Bz H H F OH XXIV-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-46-5 p-me-ph H H CH ₂ Ph Bz H H F OH XXIV-46-b p-me-ph H H CH ₂ -indol-3-yl Bz H H F OH XXIV-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-46-8 p-me-ph * H Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-47-1 p-f-ph H H H Bz H H F OH XXIV-47-2 p-f-ph H H CH ₃ Bz H H F OH XXIV-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-47-5 p-f-ph H H CH ₂ Ph Bz H H F OH XXIV-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H H F OH XXIV-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-47-8 p-f-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-48-1 p-Cl-Ph H H H Bz H H F OH XXIV-48-2 p-Cl-Ph H H CH ₃ Bz H H F OH XXIV-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-48-5 p-Cl-Ph H H CH ₂ Ph Bz H H F OH XXIV-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H H F OH XXIV-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-48-8 p-Cl-Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIV-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-49-1 p-Br-Ph H H H Bz H H F OH XXIV-49-2 p-Br-Ph H H CH ₃ Bz H H F OH XXIV-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-49-5 p-Br-Ph H H CH ₂ Ph Bz H H F OH XXIV-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H H F OH XXIV-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-49-8 p-Br-Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIV-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIV-50-1 p-i-ph H H H Bz H H F OH XXIV-50-2 p-i-ph H H CH ₃ Bz H H F OH XXIV-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXIV-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXIV-50-5 p-i-ph H H CH ₂ Ph Bz H H F OH XXIV-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H H F OH XXIV-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXIV-50-8 p-i-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-1-1 CH ₃ H H H CH ₃ N CH ₃ F IT XXV-1-2 CH ₃ H H CH ₃ CH ₃ n CH ₃ F IT XXV-1-3 CH ₃ H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-1-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-1-5 CH ₃ H H CH ₂ Ph CH ₃ n CH ₃ F IT XXV-1-6 CH ₃ H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXV-1-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXV-1-8 CH ₃ * H CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-2-1 Et H H H CH ₃ N CH ₃ F IT XXV-2-2 Et H H CH ₃ CH ₃ N CH ₃ F IT XXV-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-2-5 Et H H CH ₂ Ph CH ₃ n CH ₃ F IT XXV-2-6 Et H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXV-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXV-2-8 Et * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-3-1 ⁱ Pr N n n CH ₃ N CH ₃ F IT XXV-3-2 ⁱ Pr N n CH ₃ CH ₃ n CH ₃ F IT XXV-3-3 ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ n CH ₃ F IT XXV-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXV-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXV-3-8 ⁱ Pr * n * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-4-1 ^t Bu N n n CH ₃ N CH ₃ F IT XXV-4-2 ^t Bu N n CH ₃ CH ₃ N CH ₃ F IT XXV-4-3 ^t Bu n n CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXV-4-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXV-4-5 ^t Bu n n CH ₂ Ph CH ₃ N CH ₃ F IT XXV-4-6 ^t Bu n n CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXV-4-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT XXV-4-8 ^t Bu * n * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-5-1 Ph H H H CH ₃ N CH ₃ F IT XXV-5-2 Ph H H CH ₃ CH ₃ N CH ₃ F IT XXV-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXV-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXV-5-5 Ph H H CH ₂ Ph CH ₃ N CH ₃ F IT XXV-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXV-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT XXV-5-8 Ph * H * CH ₃ N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-6-1 p-me-ph H H H CH ₃ n CH ₃ F IT XXV-6-2 p-me-ph H H CH ₃ CH ₃ n CH ₃ F IT XXV-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F it XXV-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F it XXV-6-5 p-me-ph H H CH ₂ Ph CH ₃ n CH ₃ F it XXV-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F it XXV-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F it XXV-6-8 p-me-ph * H CH ₃ n CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-7-1 p-f-ph H H H CH ₃ n CH ₃ F IT XXV-7-2 p-f-ph H H CH ₃ CH ₃ n CH ₃ F IT XXV-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXV-7-6 p-f-ph H H CH ₂ Ph CH ₃ n CH ₃ F IT XXV-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXV-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXV-7-20 p-f-ph * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-8-1 p-Cl-Ph H H H CH ₃ H CH ₃ F OH XXV-8-2 p-Cl-Ph H H CH ₃ CH ₃ H CH ₃ F OH XXV-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXV-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXV-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ H CH ₃ F OH XXV-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXV-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXV-8-8 p-Cl-Ph * H * CH ₃ H CH ₃ F OH R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-9-1 p-Br-Ph H H H CH ₃ H CH ₃ F OH XXV-9-2 p-Br-Ph H H CH ₃ CH ₃ H CH ₃ F OH XXV-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXV-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXV-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ H CH ₃ F OH XXV-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXV-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXV-9-20 p-Br-Ph * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-10-1 p-i-ph H H H CH ₃ H CH ₃ F OH XXV-10-2 p-i-ph H H CH ₃ CH ₃ H CH ₃ F OH XXV-10-3 p-i-ph H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXV-10-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXV-10-5 p-i-ph H H CH ₂ Ph CH ₃ H CH ₃ F OH XXV-10-6 p-i-ph H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXV-10-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXV-10-8 p-i-ph * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-11-1 CH ₃ N N n Et H CH ₃ F IT XXV-11-2 CH ₃ N N CH ₃ Et H CH ₃ F IT XXV-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-11-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-11-5 CH ₃ N n CH ₂ Ph Et H CH ₃ F IT XXV-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-11-8 CH ₃ * n * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-12-1 Et H H H Et H CH ₃ F IT XXV-12-2 Et H H CH ₃ Et H CH ₃ F IT XXV-12-3 Et H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-12-5 Et H H CH ₂ Ph Et H CH ₃ F IT XXV-12-6 Et H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-12-8 Et * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-13-1 ⁱ Pr N N n Et H CH ₃ F IT XXV-13-2 ⁱ Pr N N CH ₃ Et H CH ₃ F IT XXV-13-3 ⁱ Pr N n CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-13-5 ⁱ Pr N n CH ₂ Ph Et H CH ₃ F IT XXV-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-13-8 ⁱ Pr * n * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-14-1 ^t Bu H H H Et H CH ₃ F IT XXV-14-2 ^t Bu H H CH ₃ Et H CH ₃ F IT XXV-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-14-5 ^t Bu H H CH ₂ Ph Et H CH ₃ F IT XXV-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-14-8 ^t Bu * H * Et H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-15-1 Ph H H H Et H CH ₃ F IT XXV-15-2 Ph H H CH ₃ Et H CH ₃ F IT XXV-15-3 Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-15-5 Ph H H CH ₂ Ph Et H CH ₃ F IT XXV-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-15-8 Ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-16-1 p-me-ph H H H Et H CH ₃ F IT XXV-16-2 p-me-ph H H CH ₃ Et H CH ₃ F IT XXV-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-16-5 p-me-ph H H CH ₂ Ph Et H CH ₃ F IT XXV-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-16-8 p-me-ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-17-1 p-f-ph H H H Et H CH ₃ F IT XXV-17-2 p-f-ph H H CH ₃ Et H CH ₃ F IT XXV-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ F IT XXV-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-17-8 p-f-ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-18-1 p-Cl-Ph H H H Et H CH ₃ F IT XXV-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ F IT XXV-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-18-5 p-Cl-Ph H H CH ₂ Ph Et H CH ₃ F IT XXV-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-18-8 p-Cl-Ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-19-1 p-Br-Ph H H H Et H CH ₃ F IT XXV-19-2 p-Br-Ph H H CH ₃ Et H CH ₃ F IT XXV-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXV-19-5 p-Br-Ph H H CH ₂ Ph Et H CH ₃ F IT XXV-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXV-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXV-19-8 p-Br-Ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-20-1 p-i-ph H H H Et H CH ₃ F OH XXV-20-2 p-i-ph H H CH ₃ Et H CH ₃ F OH XXV-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F OH XXV-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F OH XXV-20-5 p-i-ph H H CH ₂ Ph Et H CH ₃ F OH XXV-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H CH ₃ F OH XXV-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F OH XXV-20-8 p-i-ph * H * Et H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-21 No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-21-1 CH ₃ H H H ⁱ Pr H CH ₃ F OH XXV-21-2 CH ₃ H H CH ₃ ⁱ Pr H CH ₃ F OH XXV-21-3 CH ₃ H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-21-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-21-5 CH ₃ H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXV-21-6 CH ₃ H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXV-21-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXV-21-8 CH ₃ * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-22-1 Et H H H ⁱ Pr H CH ₃ F OH XXV-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ F OH XXV-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXV-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXV-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXV-22-8 Et * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-23-1 ⁱ Pr H H H ⁱ Pr H CH ₃ F IT XXV-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H CH ₃ F IT XXV-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXV-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXV-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXV-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXV-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXV-23-8 ⁱ Pr * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-24-1 ^t Bu N n n ⁱ Pr N CH ₃ F IT XXV-24-2 ^t Bu N n CH ₃ ⁱ Pr N CH ₃ F IT XXV-24-3 ^t Bu N n CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXV-24-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXV-24-5 ^t Bu N n CH ₂ Ph ⁱ Pr N CH ₃ F IT XXV-24-6 ^t Bu N n CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT XXV-24-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT XXV-24-8 ^t Bu * n * ⁱ Pr n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-25-1 Ph H H H ⁱ Pr H CH ₃ F IT XXV-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXV-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXV-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXV-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXV-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F it XXV-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXV-25-8 Ph * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-26-1 p-me-ph H H H ⁱ Pr H CH ₃ F OH XXV-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXV-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXV-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXV-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXV-26-8 p-me-ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-27-1 p-f-ph H H H ⁱ Pr H CH ₃ F OH XXV-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXV-27-3 p-f-ph H H CH (CH ₃ ) ₂ ipr H CH ₃ F OH XXV-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXV-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXV-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXV-27-8 p-f-ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-28-1 p-Cl-Ph H H H ⁱ Pr H CH ₃ F OH XXV-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXV-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXV-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXV-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXV-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXV-28-8 p-Cl-Ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ F IT XXV-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXV-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXV-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXV-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F it XXV-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F it XXV-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F it XXV-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-30-1 p-1-ph N N n ⁱ Pr N CH ₃ F IT XXV-30-2 p-1-ph n N CH ₃ ⁱ Pr N CH ₃ F IT XXV-30-3 p-1-ph n N CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXV-30-4 p-1-ph n N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXV-30-5 p-1-ph n n CH ₂ Ph ⁱ Pr n CH ₃ F IT XXV-30-6 p-1-ph n n CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT XXV-30-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT XXV-30-8 p-1-ph * n * ⁱ Pr n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-31-1 CH ₃ N N N ⁿ Bu H CH ₃ F IT XXV-31-2 CH ₃ N N CH ₃ ⁿ Bu H CH ₃ F IT XXV-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-31-8 CH ₃ * N * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-32-1 Et H H H ⁿ Bu H CH ₃ F IT XXV-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ F IT XXV-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-32-8 Et * H * ⁿ Bu H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-33-1 ^t Bu n n n ⁿ Bu H CH ₃ F IT XXV-33-2 ^t Bu n n CH ₃ ⁿ Bu H CH ₃ F IT XXV-33-3 ^t Bu n n CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-33-4 ^t Bu n n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-33-5 ^t Bu n n CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-33-6 ^t Bu n n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-33-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-33-8 ^t Bu * n * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-34-1 ^t Bu N n n ⁿ Bu N CH ₃ F IT XXV-34-2 ^t Bu N n CH ₃ ⁿ Bu N CH ₃ F IT XXV-34-3 ^t Bu n n CH (CH ₃ ) ₂ ⁿ Bu n CH ₃ F IT XXV-34-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu n CH ₃ F IT XXV-34-5 ^t Bu N n CH ₂ Ph ⁿ Bu n CH ₃ F IT XXV-34-6 ^t Bu N n CH ₂ -indol-3-yl ⁿ Bu n CH ₃ F IT XXV-34-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu n CH ₃ F IT XXV-34-8 ^t Bu * n * ⁿ Bu n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-35-1 Ph H H H ⁿ Bu H CH ₃ F IT XXV-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXV-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-35-8 Ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-36-1 p-me-ph H H H ⁿ Bu H CH ₃ F IT XXV-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXV-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-36-8 p-me-ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-37-1 p-f-ph H H H ⁿ Bu H CH ₃ F IT XXV-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXV-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-37-8 p-f-ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ F IT XXV-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXV-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-38-8 p-Cl-Ph H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ F IT XXV-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXV-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F it XXV-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F it XXV-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F it XXV-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F it XXV-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F it XXV-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-40-1 p-1-ph N N n ⁿ Bu H CH ₃ F IT XXV-40-2 p-1-ph N N CH ₃ ⁿ Bu H CH ₃ F IT XXV-40-3 p-1-ph N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-40-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXV-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H CH ₃ F IT XXV-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXV-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXV-40-8 p-1-ph * n * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-41-1 CH ₃ N N N Bz H CH ₃ F IT XXV-41-2 CH ₃ N n CH ₃ Bz H CH ₃ F IT XXV-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-41-5 CH ₃ N n CH ₂ Ph Bz H CH ₃ F IT XXV-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-41-8 CH ₃ * n * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-42-1 Et H H H Bz H CH ₃ F IT XXV-42-2 Et H H CH ₃ Bz H CH ₃ F IT XXV-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-42-5 Et H H CH ₂ Ph Bz H CH ₃ F IT XXV-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-42-8 Et * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-43-1 ⁱ Pr N n n Bz H CH ₃ F IT XXV-43-2 ⁱ Pr N n CH ₃ Bz H CH ₃ F IT XXV-43-3 ⁱ Pr N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-43-5 ⁱ Pr N n CH ₂ Ph Bz H CH ₃ F IT XXV-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-43-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-43-8 ⁱ Pr * n * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-44-1 ^t Bu H H H Bz H CH ₃ F IT XXV-44-2 ^t Bu H H CH ₃ Bz H CH ₃ F IT XXV-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-44-5 ^t Bu H H CH ₂ Ph Bz H CH ₃ F IT XXV-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-44-8 ^t Bu * H * Bz H CH ₃ F IT Table XXV-45. * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-45-1 Ph H H H Bz H CH ₃ F IT XXV-45-2 Ph H H CH ₃ Bz H CH ₃ F IT XXV-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-45-5 Ph H H CH ₂ Ph Bz H CH ₃ F IT XXV-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-45-8 Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-46-1 p-me-ph H H H Bz H CH ₃ F IT XXV-46-2 p-me-ph H H CH ₃ Bz H CH ₃ F IT XXV-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ F IT XXV-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-46-8 p-me-ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-47-1 p-f-ph H H H Bz H CH ₃ F IT XXV-47-2 p-f-ph H H CH ₃ Bz H CH ₃ F IT XXV-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ F IT XXV-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-47-8 p-f-ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-48-1 p-Cl-Ph H H H Bz H CH ₃ F IT XXV-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ F IT XXV-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ F IT XXV-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-48-8 p-Cl-Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXV-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-49-1 p-Br-Ph H H H Bz H CH ₃ F IT XXV-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ F IT XXV-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ F IT XXV-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-49-8 p-Br-Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXV-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV-50-1 p-i-ph H H H Bz H CH ₃ F IT XXV-50-2 p-i-ph H H CH ₃ Bz H CH ₃ F IT XXV-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXV-50-5 p-i-ph H H CH ₂ Ph Bz H CH ₃ F IT XXV-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXV-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXV-50-8 p-i-ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-1-1 CH ₃ N N n CH ₃ n F N IT XXVI-1-2 CH ₃ N N CH ₃ CH ₃ n F N IT XXVI-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ n F N IT XXVI-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT XXVI-1-5 CH ₃ N n CH ₂ Ph CH ₃ n F N IT XXVI-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ n F N IT XXVI-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT XXVI-1-8 CH ₃ * n * CH ₃ n F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-2-1 Et H H H CH ₃ H F H OH XXVI-2-2 Et H H CH ₃ CH ₃ H F H OH XXVI-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H F H OH XXVI-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F H OH XXVI-2-5 Et H H CH ₂ Ph CH ₃ H F H OH XXVI-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H F H OH XXVI-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H F H OH XXVI-2-8 Et * H * CH ₃ H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-3-1 ⁱ Pr H H H CH ₃ H F H OH XXVI-3-2 ⁱ Pr H H CH ₃ CH ₃ H F H OH XXVI-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ H F H OH XXVI-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F H OH XXVI-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ H F H OH XXVI-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ H F H OH XXVI-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ H F H OH XXVI-3-8 ⁱ Pr * H * CH ₃ H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XX \ 1-4-1 ^t Bu H H H CH ₃ H F H OH XXVI-4-2 ^t Bu H H CH ₃ CH ₃ H F H OH XXVI-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ H F H OH XXVI-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F H OH XXVI-4-5 ^t Bu H H CH ₂ Ph CH ₃ H F H OH XXVI-4-b ^t Bu H H CH ₂ -indol-3-yl CH ₃ H F H OH XXVI-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ H F H OH XXVI-4-8 ^t Bu * H * CH ₃ H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-5-1 Ph H H H CH ₃ N F n IT XXVI-5-2 Ph H H CH ₃ CH ₃ N F n it XXVI-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ N F n it XXVI-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXVI-5-5 Ph H H CH ₂ Ph CH ₃ N F n it XXVI-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ N F n it XXVI-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it XXVI-5-8 Ph * H * CH ₃ N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-6-1 p-me-ph H H H CH ₃ n F N IT XXVI-6-2 p-me-ph H H CH ₃ CH ₃ n F N IT XXVI-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ n F N IT XXVI-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT XXVI-6-5 p-me-ph H H CH ₂ Ph CH ₃ n F N IT XXVI-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n F N IT XXVI-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT XXVI-6-8 p-me-ph * H * CH ₃ n F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-7-1 p-f-ph H H H CH ₃ N F n IT XXVI-7-2 p-f-ph H H CH ₃ CH ₃ N F n it XXVI-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N F n it XXVI-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXVT-7-6 p-f-ph H H CH ₂ Ph CH ₃ N F n it XXVI-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N F n it XXVI-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXVI-7-20 p-f-ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-8.

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-8-1 p-Cl-Ph H H H CH ₃ N F n IT XXV1-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F n IT XXV1-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ n F n it XXVI-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it XXVI-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n F n it XXVI-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n F n it XXVI-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXVI-8-8 p-Cl-Ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-9-1 p-Br-Ph H H H CH ₃ N F n IT XXV1-9-2 p-Br-Ph H H CH ₃ CH ₃ N F n IT XXVI-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F n it XXV1-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it XXVI-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F n it XXVI-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n F n it XXVI-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXVI-9-20 p-Br-Ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV1-10-1 p-1-ph N n n CH ₃ N F N IT XXVI-10-2 p-1-ph N n CH ₃ CH ₃ N F N IT XXV1-10-3 p-1-ph n n CH (CH ₃ ) ₂ CH ₃ N F N IT XXV1-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT XXVI-10-5 p-1-ph n n CH ₂ Ph CH ₃ N F N IT XXVI-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N F N IT XXVI-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT XXVI-10-8 p-1-ph * n * CH ₃ N F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-11 No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-11-1 CH ₃ N N N Et H F H OH XXVI-11-2 CH ₃ N N CH ₃ Et H F H OH XXVI-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H F H OH XXVI-11-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-11-5 CH ₃ N N CH ₂ Ph Et H F H OH XXVI-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H F H OH XXVI-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-11-8 CH ₃ * n Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-12-1 Et H H H Et H F H OH XXVI-12-2 Et H H CH ₃ Et H F H OH XXVI-12-3 Et H H CH (CH ₃ ) ₂ Et H F H OH XXVI-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-12-5 Et H H CH ₂ Ph Et H F H OH XXVI-12-6 Et H H CH ₂ -indol-3-yl Et H F H OH XXVI-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-12-8 Et * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-13-1 ⁱ Pr H H H Et H F H OH XXVI-13-2 ⁱ Pr H H CH ₃ Et H F H OH XXVI-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et H F H OH XXVI-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-13-5 ⁱ Pr H H CH ₂ Ph Et H F H OH XXVI-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et H F H OH XXVI-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-13-8 ⁱ Pr * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-14-1 ^t Bu H H H Et H F H OH XXVI-14-2 ^t Bu H H CH ₃ Et H F H OH XXVI-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H F H OH XXV1-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-14-5 ^t Bu H H CH ₂ Ph Et H F H OH XXVI-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H F H OH XXVI-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-14-8 ^t Bu * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-15-1 Ph H H H Et H F H OH XXVI-15-2 Ph H H CH ₃ Et H F H OH XXVI-15-3 Ph H H CH (CH ₃ ) ₂ Et H F H OH XXVI-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-15-5 Ph H H CH ₂ Ph Et H F H OH XXVI-15-6 Ph H H CH ₂ -indol-3-yl Et H F H OH XXVI-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-15-8 Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-16-1 p-me-ph H H H Et H F H OH XXVI-16-2 p-me-ph H H CH ₃ Et H F H OH XXVI-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F H OH XXVI-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-16-5 p-me-ph H H CH ₂ Ph Et H F H OH XXVI-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F H OH XXVI-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-16-8 p-me-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-17-1 p-f-ph H H H Et H F H OH XXVI-17-2 p-f-ph H H CH ₃ Et H F H OH XXVI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F H OH XXVI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-17-5 p-f-ph H H CH ₂ Ph Et H F H OH XXVI-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F H OH XXVI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-17-8 p-f-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-18-1 p-Cl-Ph H H H Et H F H OH XXVI-18-2 p-Cl-Ph H H CH ₃ Et H F H OH XXVI-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F H OH XXVI-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-18-5 p-Cl-Ph H H CH ₂ Ph Et H F H OH XXVI-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F H OH XXVI-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-18-8 p-Cl-Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-19-1 p-Br-Ph H H H Et H F H OH XXVI-19-2 p-Br-Ph H H CH ₃ Et H F H OH XXVI-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F H OH XXVI-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-19-5 p-Br-Ph H H CH ₂ Ph Et H F H OH XXVI-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F H OH XXVI-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-19-8 p-Br-Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-20-1 p-i-ph H H H Et H F H OH XXVI-20-2 p-i-ph H H CH ₃ Et H F H OH XXVI-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H F H OH XXVI-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXVI-20-5 p-i-ph H H CH ₂ Ph Et H F H OH XXVI-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H F H OH XXVI-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXVI-20-8 p-i-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-21-1 CH ₃ H H H ⁱ Pr H F H OH XXVI-21-2 CH ₃ H H CH ₃ ⁱ Pr H F H OH XXVI-21-3 CH ₃ H H CH (CH ₃ ) ₂ Tt H F H OH XXVI-21-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-21-5 CH ₃ H H CH ₂ Ph ⁱ Pr H F H OH XXVI-21-6 CH ₃ H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-21-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-21-8 CH ₃ * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-22-1 Et H H H ⁱ Pr H F H OH XXVI-22-2 Et H H CH ₃ ⁱ Pr H F H OH XXVI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVT-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-22-5 Et H H CH ₂ Ph ⁱ Pr H F H OH XXVI-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-22-8 Et * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-23-1 ⁱ Pr H H H ⁱ Pr H F H OH XXVI-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H F H OH XXVI-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H F H OH XXVI-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVT-23-8 ⁱ Pr * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-24-1 ^t Bu H H H ⁱ Pr H F H OH XXVI-24-2 ^t Bu H H CH ₃ * Rg H F H OH XXVI-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H F H OH XXVI-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-24-8 ^t Bu * H * * Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-25-1 Ph H H H ⁱ Pr H F H OH XXVI-25-2 Ph H H CH ₃ ⁱ Pr H F H OH XXVI-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-25-5 Ph H H CH ₂ Ph ⁱ Pr H F H OH XXVI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-25-8 Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-26-1 p-me-ph H H H ⁱ Pr H F H OH XXVI-26-2 p-me-ph H H CH ₃ ⁱ Pr H F H OH XXVI-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F H OH XXVI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-26-8 p-me-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-27-1 p-f-ph H H H ⁱ Pr H F H OH XXVI-27-2 p-f-ph H H CH ₃ ⁱ Pr H F H OH XXVI-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F H OH XXVI-27-b p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVT-27-8 p-f-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-28-1 p-Cl-Ph H H H ⁱ Pr H F H OH XXVI-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F H OH XXVI-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F H OH XXVI-28-b p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-28-8 p-Cl-Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-29-1 p-Br-Ph H H H ⁱ Pr H F H OH XXVI-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F H OH XXVI-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F H OH XXVI-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-29-8 p-Br-Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-30-1 p-i-ph H H H ⁱ Pr H F H OH XXVI-30-2 p-i-ph H H CH ₃ ⁱ Pr H F H OH XXVI-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXVI-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H F H OH XXVI-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXVI-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXVI-30-8 p-i-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-31 No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-31-1 CH ₃ H H H ⁿ Bu H F H OH XXVI-31-2 CH ₃ H H CH ₃ ⁿ Bu H F H OH XXVI-31-3 CH ₃ H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-31-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-31-5 CH ₃ H H CH ₂ Ph ⁿ Bu H F H OH XXVI-31-6 CH ₃ H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-31-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-31-8 CH ₃ * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-32-1 Et H H H ⁿ Bu H F H OH XXVI-32-2 Et H H CH ₃ ⁿ Bu H F H OH XXVI-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-32-5 Et H H CH ₂ Ph ⁿ Bu H F H OH XXVI-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-32-8 Et * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-33-1 ⁱ Pr H H H ⁿ Bu H F H OH XXVI-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H F H OH XXVI-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H F H OH XXVI-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-33-8 ⁱ Pr * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-34-1 ^t Bu H H H ⁿ Bu H F H OH XXVI-34-2 ^t Bu H H CH ₃ ⁿ Bu H F H OH XXVI-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H F H OH XXVI-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-34-8 ^t Bu * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-35-1 Ph H H H ⁿ Bu H F H OH XXVI-35-2 Ph H H CH ₃ ⁿ Bu H F H OH XXVI-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-35-5 Ph H H CH ₂ Ph ⁿ Bu H F H OH XXVI-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-35-8 Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-36-1 p-me-ph H H H ⁿ Bu H F H OH XXVI-36-2 p-me-ph H H CH ₃ ⁿ Bu H F H OH XXVI-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F H OH XXVI-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-36-8 p-me-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-37-1 p-f-ph H H H ⁿ Bu H F H OH XXVI-37-2 p-f-ph H H CH ₃ ⁿ Bu H F H OH XXVI-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVT-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F H OH XXVI-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVT-37-8 p-f-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-38-1 p-Cl-Ph H H H ⁿ Bu H F H OH XXVI-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F H OH XXVI-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F H OH XXVI-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-38-8 p-Cl-Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-39-1 p-Br-Ph H H H ⁿ Bu H F H OH XXVI-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F H OH XXVI-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVT-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F H OH XXVI-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-39-8 p-Br-Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-40-1 p-i-ph H H H ⁿ Bu H F H OH XXVI-40-2 p-i-ph H H CH ₃ ⁿ Bu H F H OH XXVI-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXVI-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H F H OH XXVI-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXVI-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXVI-40-8 p-i-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-41-1 CH ₃ N n n Bz H F H OH XXVI-41-2 CH ₃ N n CH ₃ Bz H F H OH XXVI-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H F H OH XXVI-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-41-5 CH ₃ N n CH ₂ Ph Bz H F H OH XXVI-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H F H OH XXVI-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-41-8 CH ₃ * n * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-42-1 Et H H H Bz H F H OH XXVI-42-2 Et H H CH ₃ Bz H F H OH XXVI-42-3 Et H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-42-5 Et H H CH ₂ Ph Bz H F H OH XXVI-42-6 Et H H CH ₂ -indol-3-yl Bz H F H OH XXVI-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-42-8 Et * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-43-1 ⁱ Pr H H H Bz H F H OH XXVI-43-2 ⁱ Pr H H CH ₃ Bz H F H OH XXVT-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-43-5 ⁱ Pr H H CH ₂ Ph Bz H F H OH XXVI-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H F H OH XXVI-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-43-8 ⁱ Pr * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-44-1 ^t Bu H H H Bz H F H OH XXVI-44-2 ^t Bu H H CH ₃ Bz H F H OH XXVI-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-44-5 ^t Bu H H CH ₂ Ph Bz H F H OH XXVI-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H F H OH XXVI-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-44-8 ^t Bu * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-45-1 Ph H H H Bz H F H OH XXVI-45-2 Ph H H CH ₃ Bz H F H OH XXVI-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXVT-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-45-5 Ph H H CH ₂ Ph Bz H F H OH XXVI-45-6 Ph H H CH ₂ -indol-3-yl Bz H F H OH XXVI-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-45-8 Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-46-1 p-me-ph H H H Bz H F H OH XXVI-46-2 p-me-ph H H CH ₃ Bz H F H OH XXVI-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-46-5 p-me-ph H H CH ₂ Ph Bz H F H OH XXVT-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F H OH XXVI-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-46-8 p-me-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-47-1 p-f-ph H H H Bz H F H OH XXVI-47-2 p-f-ph H H CH ₃ Bz H F H OH XXVI-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-47-5 p-f-ph H H CH ₂ Ph Bz H F H OH XXVI-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F H OH XXVI-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-47-8 p-f-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-48-1 p-Cl-Ph H H H Bz H F H OH XXVI-48-2 p-Cl-Ph H H CH ₃ Bz H F H OH XXVI-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXVT-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F H OH XXVI-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F H OH XXVI-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-48-8 p-Cl-Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVI-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVI-49-1 p-Br-Ph H H H Bz H F H OH XXVT-49-2 p-Br-Ph H H CH ₃ Bz H F H OH XXVI-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-49-5 p-Br-Ph H H CH ₂ Ph Bz H F H OH XXVI-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F H OH XXVI-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-49-8 p-Br-Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVI-50. No. R R Rja Rjb R R R X Y XXVI-50-1 p-i-ph H H H Bz H F H OH XXVI-50-2 p-i-ph H H CH ₃ Bz H F H OH XXVI-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXVI-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXVI-50-5 p-i-ph H H CH ₂ Ph Bz H F H OH XXVI-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H F H OH XXVI-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXVI-50-8 p-i-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-1 No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-1-1 CH ₃ N n n CH ₃ N F F IT XXVII-1-2 CH ₃ N n CH ₃ CH ₃ N F F IT XXVII-1-3 CH ₃ n n CH (CH ₃ ) ₂ CH ₃ n F F IT XXVII-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT XXVII-1-5 CH ₃ n n CH ₂ Ph CH ₃ n F F IT XXVII-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ n F F IT XXVH-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXVII-1-8 CH ₃ * n * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXV1I-2-1 Et H H H CH ₃ H F F OH XXVII-2-2 Et H H CH ₃ CH ₃ H F F OH XXVII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-2-5 Et H H CH ₂ Ph CH ₃ H F F OH XXVII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H F F OH XXVII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXVII-2-8 Et * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-3-1 ⁱ Pr H H H CH ₃ H F F OH XXVII-3-2 ⁱ Pr H H CH ₃ CH ₃ H F F OH XXVII-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ H F F OH XXVTI-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ H F F OH XXVII-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXVII-3-8 ⁱ Pr * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-4-1 ^t Bu H H H CH ₃ H F F OH XXVII-4-2 ^t Bu H H CH ₃ CH ₃ H F F OH XXVII-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-4-5 ^t Bu H H CH ₂ Ph CH ₃ H F F OH XXVII-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ H F F OH XXVII-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXVII-4-8 ^t Bu * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-5-1 Ph H H H CH ₃ H F F OH XXVII-5-2 Ph H H CH ₃ CH ₃ H F F OH XXVII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-5-5 Ph H H CH ₂ Ph CH ₃ H F F OH XXVH-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ H F F OH XXVTI-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXVII-5-8 Ph * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-6-1 p-me-ph H H H CH ₃ H F F OH XXVII-6-2 p-me-ph H H CH ₃ CH ₃ H F F OH XXVII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-6-5 p-me-ph H H CH ₂ Ph CH ₃ H F F OH XXVII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ H F F OH XXVII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXVII-6-8 p-me-ph * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-7-1 p-f-ph H H H CH ₃ H F F OH XXVII-7-2 p-f-ph H H CH ₃ CH ₃ H F F OH XXVII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXVII-7-6 p-f-ph H H CH ₂ Ph CH ₃ H F F OH XXVII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ H F F OH XXVII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXVH-7-20 p-f-ph * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-8-1 p-Cl-Ph H H H CH ₃ N F F IT XXVII-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F F IT XXVII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT XXVII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT XXVII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n F F IT XXVII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n F F IT XXVII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXVII-8-8 p-Cl-Ph * H CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-9-1 p-Br-Ph H H H CH ₃ N F F IT XXVII-9-2 p-Br-Ph H H CH ₃ CH ₃ N F F IT XXVII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT XXVII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT XXVII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F F IT XXVII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N F F IT XXVII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT XXVH-9-20 p-Br-Ph * H * CH ₃ N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVTI-10-1 p-1-ph N n n CH ₃ N F F IT XXVII-10-2 p-1-ph N n CH ₃ CH ₃ N F F IT XXVII-10-Z p-1-ph n n CH (CH ₃ ) ₂ CH ₃ N F F IT XXVTI-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT XXVII-10-5 p-1-ph n n CH ₂ Ph CH ₃ N F F IT XXVH-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N F F IT XXVII-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT XXVII-10-8 p-1-ph * n * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-11-1 CH ₃ N N n Et H F F OH XXVII-11-2 CH ₃ N N CH ₃ Et H F F OH XXVH-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H F F OH XXVII-11-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-11-5 CH ₃ N N CH ₂ Ph Et H F F OH XXVII-11-b CH ₃ N N CH ₂ -indol-3-yl Et H F F OH XXVII-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-11-8 CH ₃ * N * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-12-1 Et H H H Et H F F OH XXVII-12-2 Et H H CH ₃ Et H F F OH XXVII-12-3 Et H H CH (CH ₃ ) ₂ Et H F F OH XXVII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-12-5 Et H H CH ₂ Ph Et H F F OH XXVII-12-6 Et H H CH ₂ -indol-3-yl Et H F F OH XXVII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-12-8 Et * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-13-1 ⁱ Pr H H H Et H F F OH XXVII-13-2 ⁱ Pr H H CH ₃ Et H F F OH XXVII-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et H F F OH XXVII-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-13-5 ⁱ Pr H H CH ₂ Ph Et H F F OH XXVII-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et H F F OH XXVII-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-13-8 ⁱ Pr * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-14-1 ^t Bu H H H Et H F F OH XXVII-14-2 ^t Bu H H CH ₃ Et H F F OH XXVII-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H F F OH XXVII-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-14-5 ^t Bu H H CH ₂ Ph Et H F F OH XXVII-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H F F OH XXVII-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-14-8 ^t Bu * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-15-1 Ph H H H Et H F F OH XXVII-15-2 Ph H H CH ₃ Et H F F OH XXVII-15-3 Ph H H CH (CH ₃ ) ₂ Et H F F OH XXVII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-15-5 Ph H H CH ₂ Ph Et H F F OH XXVII-15-6 Ph H H CH ₂ -indol-3-yl Et H F F OH XXVII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-15-8 Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-16-1 p-me-ph H H H Et H F F OH XXVII-16-2 p-me-ph H H CH ₃ Et H F F OH XXVII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F F OH XXVII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-16-5 p-me-ph H H CH ₂ Ph Et H F F OH XXVII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F F OH XXVII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-16-8 p-me-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-17-1 p-f-ph H H H Et H F F OH XXVII-17-2 p-f-ph H H CH ₃ Et H F F OH XXVII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F F OH XXVTI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVTI-17-5 p-f-ph H H CH ₂ Ph Et H F F OH XXVII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F F OH XXVII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-17-8 p-f-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-18-1 p-Cl-Ph H H H Et H F F OH XXVII-18-2 p-Cl-Ph H H CH ₃ Et H F F OH XXVII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F F OH XXVII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVH-18-5 p-Cl-Ph H H CH ₂ Ph Et H F F OH XXVII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F F OH XXVII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-18-8 p-Cl-Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVH-19-1 p-Br-Ph H H H Et H F F OH XXVII-19-2 p-Br-Ph H H CH ₃ Et H F F OH XXVII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F F OH XXVII-19-4 p-Br-Ph H. H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-19-5 p-Br-Ph H H CH ₂ Ph Et H F F OH XXV1I-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F F OH XXVII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-19-8 p-Br-Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-20-1 p-i-ph H H H Et H F F OH XXVII-20-2 p-i-ph H H CH ₃ Et H F F OH XXVII-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H F F OH XXVII-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXVII-20-5 p-i-ph H H CH ₂ Ph Et H F F OH XXVII-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H F F OH XXVII-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXVII-20-8 p-i-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-21-1 CH ₃ N n n ⁱ Pr N F F IT XXVII-21-2 CH ₃ N n CH ₃ ⁱ Pr n F F IT XXVII-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr n F F IT XXVII-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F F IT XXVII-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr n F F IT XXVII-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr n F F IT XXVII-21-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F F IT XXVII-21-8 CH ₃ * n * ⁱ Pr n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-22-1 Et H H H ⁱ Pr H F F OH XXVII-22-2 Et H H CH ₃ ⁱ Pr H F F OH XXVII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVH-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVH-22-5 Et H H CH ₂ Ph ⁱ Pr H F F OH XXVII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-22-8 Et * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-23-1 ⁱ Pr H H H ⁱ Pr H F F OH XXVII-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H F F OH XXVII-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H F F OH XXVII-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-23-8 ⁱ Pr * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-24-1 ^t Bu H H H ⁱ Pr H F F OH XXVII-24-2 ^t Bu H H CH ₃ ⁱ Pr H F F OH XXVII-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVH-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H F F OH XXVII-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-24-8 ^t Bu * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-25-1 Ph H H H ⁱ Pr H F F OH XXVII-25-2 Ph H H CH ₃ ⁱ Pr H F F OH XXVII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-25-5 Ph H H CH ₂ Ph ⁱ Pr H F F OH XXVII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-25-8 Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-26-1 p-me-ph H H H ⁱ Pr H F F OH XXVII-26-2 p-me-ph H H CH ₃ ⁱ Pr H F F OH XXVII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F F OH XXVII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-26-8 p-me-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-27-1 p-f-ph H H H ⁱ Pr H F F OH XXVII-27-2 p-f-ph H H CH ₃ ⁱ Pr H F F OH XXVII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F F OH XXVII-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-27-8 p-f-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-28-1 p-Cl-Ph H H H ⁱ Pr H F F OH XXVII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F F OH XXVII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ H F F OH XXVII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F F OH XXVTI-28-6 p-Cl-Ph H H CH ₂ -ind ol-3-yl ⁱ Pr H F F OH XXVII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-28-8 p-Cl-Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-29-1 p-Br-Ph H H H ⁱ Pr H F F OH XXVII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F F OH XXVII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVH-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F F OH XXVII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-29-8 p-Br-Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-30-1 p-i-ph H H H ⁱ Pr H F F OH XXVII-30-2 p-i-ph H H CH ₃ ⁱ Pr H F F OH XXVII-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXVII-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H F F OH XXVII-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXVII-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXVII-30-8 p-i-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-31-1 CH ₃ N N n ⁿ Bu H F F OH XXVII-31-2 CH ₃ N N CH ₃ ⁿ Bu H F F OH XXVII-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H F F OH XXVII-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-31-8 CH ₃ * N * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-32-1 Et H H H ⁿ Bu H F F OH XXVII-32-2 Et H H CH ₃ ⁿ Bu H F F OH XXVII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-32-5 Et H H CH ₂ Ph ⁿ Bu H F F OH XXVII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-32-8 Et * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-33-1 ⁱ Pr H H H ⁿ Bu H F F OH XXVII-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H F F OH XXVII-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H F F OH XXVII-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-33-8 ⁱ Pr * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-34-1 ^t Bu H H H ⁿ Bu H F F OH XXVII-34-2 ^t Bu H H CH ₃ ⁿ Bu H F F OH XXVII-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H F F OH XXVII-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-34-8 ^t Bu * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-35-1 Ph H H H ⁿ Bu H F F OH XXVII-35-2 Ph H H CH ₃ ⁿ Bu H F F OH XXVII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-35-5 Ph H H CH ₂ Ph ⁿ Bu H F F OH XXVII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-35-8 Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-36-1 p-me-ph H H H ⁿ Bu H F F OH XXVII-36-2 p-me-ph H H CH ₃ ⁿ Bu H F F OH XXVII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F F OH XXVII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-36-8 p-me-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-37-1 p-f-ph H H H ⁿ Bu H F F OH XXVII-37-2 p-f-ph H H CH ₃ ⁿ Bu H F F OH XXVII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F F OH XXVII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-37-8 p-f-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-38-1 p-Cl-Ph H H H ⁿ Bu H F F OH XXVII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F F OH XXVII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F F OH XXVII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-38-8 p-Cl-Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-39-1 p-Br-Ph H H H ⁿ Bu H F F OH XXVII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F F OH XXVII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F F OH XXVII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-39-8 p-Br-Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-40-1 p-i-ph H H H ⁿ Bu H F F OH XXVII-40-2 p-i-ph H H CH ₃ ⁿ Bu H F F OH XXVII-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXVII-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H F F OH XXVII-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXVII-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXVII-40-8 p-i-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-41-1 CH ₃ N N n Bz H F F OH XXVII-41-2 CH ₃ N N CH ₃ Bz H F F OH XXVII-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H F F OH XXVII-41-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-41-5 CH ₃ N n CH ₂ Ph Bz H F F OH XXVII-41-6 CH ₃ N N CH ₂ -indol-3-yl Bz H F F OH XXVII-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-41-8 CH ₃ * n * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-42-1 Et H H H Bz H F F OH XXVII-42-2 Et H H CH ₃ Bz H F F OH XXVII-42-3 Et H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-42-5 Et H H CH ₂ Ph Bz H F F OH XXVII-42-6 Et H H CH ₂ -indol-3-yl Bz H F F OH XXVII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-42-8 Et * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-43-1 ⁱ Pr H H H Bz H F F OH XXVII-43-2 ⁱ Pr H H CH ₃ Bz H F F OH XXVII-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-43-5 ⁱ Pr H H CH ₂ Ph Bz H F F OH XXVII-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H F F OH XXVII-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-43-8 ⁱ Pr * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-44-1 ^t Bu H H H Bz H F F OH XXVII-44-2 ^t Bu H H CH ₃ Bz H F F OH XXV1I-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-44-5 ^t Bu H H CH ₂ Ph Bz H F F OH XXVII-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H F F OH XXVII-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-44-8 ^t Bu * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-45-1 Ph H H H Bz H F F OH XXVII-45-2 Ph H H CH ₃ Bz H F F OH XXVII-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-45-5 Ph H H CH ₂ Ph Bz H F F OH XXVII-45-6 Ph H H CH ₂ -indol-3-yl Bz H F F OH XXVII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-45-8 Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-46-1 p-me-ph H H H Bz H F F OH XXVII-46-2 p-me-ph H H CH ₃ Bz H F F OH XXVII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-46-5 p-me-ph H H CH ₂ Ph Bz H F F OH XXVII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F F OH XXVII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-46-8 p-me-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-47-1 p-f-ph H H H Bz H F F OH XXVII-47-2 p-f-ph H H CH ₃ Bz H F F OH XXVII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-47-5 p-f-ph H H CH ₂ Ph Bz H F F OH XXVII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F F OH XXVII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-47-8 p-f-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-48-1 p-Cl-Ph H H H Bz H F F OH XXVII-48-2 p-Cl-Ph H H CH ₃ Bz H F F OH XXVII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F F OH XXVII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F F OH XXVII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-48-8 p-Cl-Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-49-1 p-Br-Ph H H H Bz H F F OH XXVII-49-2 p-Br-Ph H H CH ₃ Bz H F F OH XXVII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-49-5 p-Br-Ph H H CH ₂ Ph Bz H F F OH XXVII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F F OH XXVII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-49-8 p-Br-Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVII-50-1 p-i-ph H H H Bz H F F OH XXVII-50-2 p-i-ph H H CH ₃ Bz H F F OH XXVII-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXVII-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXVII-50-5 p-i-ph H H CH ₂ Ph Bz H F F OH XXVII-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H F F OH XXVII-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXVII-50-8 p-i-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-1-1 CH ₃ N N n CH ₃ N N F IT XXVIII-1-2 CH ₃ N n CH ₃ CH ₃ N N F IT XXVIII-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-1-5 CH ₃ N n CH ₂ Ph CH ₃ N N F IT XXVIII-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ N N F IT XXVIII-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT XXVIII-1-8 CH ₃ * n * CH ₃ N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-2-1 Et H H H CH ₃ N N F IT XXVIII-2-2 Et H H CH ₃ CH ₃ N N F IT XXVIII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-2-5 Et H H CH ₂ Ph CH ₃ N N F IT XXVIII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N N F IT XXVIII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT XXVIII-2-8 Et * H * CH ₃ N n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-3-1 ⁱ Pr N n n CH ₃ N N F IT XXVIII-3-2 ⁱ Pr N n CH ₃ CH ₃ N N F IT XXVIII-3-3 ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ N N F IT XXVIII-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ N N F IT XXVIII-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n N F IT XXVIII-3-8 ⁱ Pr * n * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-4-1 ^t Bu H H H CH ₃ N N F IT XXVIII-4-2 ^t Bu H H CH ₃ CH ₃ n N F IT XXVIII-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ n n F IT XXVIII-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F it XXVIII-4-5 ^t Bu H H CH ₂ Ph CH ₃ n n F it XXVIII-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ n n F it XXVIII-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F it XXYIII-4-8 ^t Bu * H * CH ₃ n n F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-5-1 Ph H H H CH ₃ n n F IT XXVIII-5-2 Ph H H CH ₃ CH ₃ n n F IT XXVIII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n n F IT XXVIII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT XXVIII-5-5 Ph H H CH ₂ Ph CH ₃ n n F IT XXVIII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n n F IT XXVIII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXVIII-5-8 Ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-6-1 p-me-ph H H H CH ₃ N n F IT XXVIII-6-2 p-me-ph H H CH ₃ CH ₃ n n F IT XXVIII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ n n F IT XXVIII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT XXVIII-6-5 p-me-ph H H CH ₂ Ph CH ₃ n n F IT XXVIII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ n n F IT XXVIII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXVIII-6-8 p-me-ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-7-1 p-f-ph H H H CH ₃ N N F IT XXVIII-7-2 p-f-ph H H CH ₃ CH ₃ N N F IT XXVIII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ N n F IT XXVIII-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT XXVIII-7-6 p-f-ph H H CH ₂ Ph CH ₃ N n F IT XXVIII-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ N n F IT XXVIII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT XXVIII-7-20 p-f-ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-8-1 p-Cl-Ph H H H CH ₃ N N F IT XXVIII-8-2 p-Cl-Ph H H CH ₃ CH ₃ N n F IT XXVIII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N n F IT XXVIII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n n F IT XXVIII-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ n n F IT XXVIII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ n n F IT XXVIII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXVIII-8-8 p-Cl-Ph * H * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-9-1 p-Br-Ph H H H CH ₃ N N F IT XXVIII-9-2 p-Br-Ph H H CH ₃ CH ₃ N N F IT XXVIII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N N F IT XXVIII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N N F IT XXVIII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT XXVIII-9-20 p-Br-Ph * H * CH ₃ N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-10-1 p-1-ph N n n CH ₃ N N F IT XXVIII-10-2 p-1-ph N n CH ₃ CH ₃ N N F IT XXVIII-10-3 p-1-ph N n CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXVIII-10-5 p-1-ph N n CH ₂ Ph CH ₃ n N F IT XXVIII-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ n N F IT XXVIII-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ n n F IT XXVIII-10-8 p-1-ph * n * CH ₃ n n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-11-1 CH ₃ N n n Et H H F OH XXVIII-11-2 CH ₃ N n CH ₃ Et H H F OH XXVIII-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H H F OH XXVIII-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-11-S CH ₃ N n CH ₂ Ph Et H H F OH XXVIII-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H H F OH XXVIII-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-11-8 CH ₃ * n * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-12-1 Et H H H Et H H F OH XXVIII-12-2 Et H H CH ₃ Et H H F OH XXVIII-12-3 Et H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-12-5 Et H H CH ₂ Ph Et H H F OH XXVIII-12-6 Et H H CH ₂ -indol-3-yl Et H H F OH XXVIII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-12-8 Et * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-13-1 ⁱ Pr H H H Et H H F OH XXVIII-13-2 ⁱ Pr H H CH ₃ Et H H F OH XXVIII-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-13-5 ⁱ Pr H H CH ₂ Ph Et H H F OH XXVIII-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et H H F OH XXVIII-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-13-8 ⁱ Pr * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-14-1 ^t Bu H H H Et H H F OH XXVIII-14-2 ^t Bu H H CH ₃ Et H H F OH XXVIII-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-14-5 ^t Bu H H CH ₂ Ph Et H H F OH XXVIII-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H H F OH XXVIII-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-14-8 ^t Bu * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-15-1 Ph H H H Et H H F OH XXVIII-15-2 Ph H H CH ₃ Et H H F OH XXVIII-15-3 Ph H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-15-5 Ph H H CH ₂ Ph Et H H F OH XXVIII-15-6 Ph H H CH ₂ -indol-3-yl Et H H F OH XXVIII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-15-8 Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-16-1 p-me-ph H H H Et H H F OH XXVIII-16-2 p-me-ph H H CH ₃ Et H H F OH XXVIII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-16-5 p-me-ph H H CH ₂ Ph Et H H F OH XXVIII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H H F OH XXVIII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-16-8 p-me-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-17-1 p-f-ph H H H Et H H F OH XXVIII-17-2 p-f-ph H H CH ₃ Et H H F OH XXVIII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-17-5 p-f-ph H H CH ₂ Ph Et H H F OH XXVIII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H H F OH XXVIII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-17-8 p-f-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-18-1 p-Cl-Ph H H H Et H H F OH XXVIII-18-2 p-Cl-Ph H H CH ₃ Et H H F OH XXVIII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-18-5 p-Cl-Ph H H CH ₂ Ph Et H H F OH XXVIII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H H F OH XXVIII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-18-8 p-Cl-Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-19-1 p-Br-Ph H H H Et H H F OH XXVIII-19-2 p-Br-Ph H H CH ₃ Et H H F OH XXVIII-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-19-5 p-Br-Ph H H CH ₂ Ph Et H H F OH XXVIII-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H H F OH XXVIII-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-19-8 p-Br-Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-20-1 p-i-ph H H H Et H H F OH XXVIII-20-2 p-i-ph H H CH ₃ Et H H F OH XXVIII-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H H F OH XXVIII-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXVIII-20-5 p-i-ph H H CH ₂ Ph Et H H F OH XXVIII-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H H F OH XXVIII-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXVIII-20-8 p-i-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-21-1 CH ₃ H H H ⁱ Pr H H F OH XXVIII-21-2 CH ₃ H H CH ₃ ⁱ Pr H H F OH XXVIII-21-3 CH ₃ H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-21-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-21-5 CH ₃ H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-21-6 CH ₃ H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-21-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-21-8 CH ₃ * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-22-1 Et H H H ⁱ Pr H H F OH XXVIII-22-2 Et H H CH ₃ ⁱ Pr H H F OH XXVIII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-22-5 Et H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-22-8 Et * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-23. No. R R Rja Rib R Rb R X Y XXVIII-23-1 ⁱ Pr H H H ⁱ Pr H H F OH XXVIII-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H H F OH XXVIII-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-23-8 ⁱ Pr * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-24-1 ^t Bu H H H ⁱ Pr H H F OH XXVIII-24-2 ^t Bu H H CH ₃ ⁱ Pr H H F OH XXVIII-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ * Pr H H F OH XXVIII-24-8 ^t Bu * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-25-1 Ph H H H ⁱ Pr H H F OH XXVIII-25-2 Ph H H CH ₃ ⁱ Pr H H F OH XXVIII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVHI-25-5 Ph H H CH ₂ Ph ⁱ Pr H H F OH XXVHI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-25-8 Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-26-1 p-me-ph H H H ⁱ Pr H H F OH XXVIII-26-2 p-me-ph H H CH ₃ ⁱ Pr H H F OH XXVIII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H H F OH XXVHI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVHI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-26-8 p-me-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-27-1 p-f-ph H H H ⁱ Pr H H F OH XXVIII-27-2 p-f-ph H H CH ₃ fpr H H F OH XXVIII-27-3 p-f-ph H H CH (CH ₃ ) ₂ * Pr H H F OH XXVIII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ * Pr H H F OH XXVIII-27-5 p-f-ph H H CH ₂ Ph * Pr H H F OH XXVIII-27-6 p-f-ph H H CH ₂ -indol-3-yl * Pr H H F OH XXVIII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ * Pr H H F OH XXVIII-27-8 p-f-ph * H ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-28-1 p-Cl-Ph H H H ⁱ Pr H H F OH XXVIII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H H F OH XXVIII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXV1II-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-28-8 p-Cl-Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-29-1 p-Br-Ph H H H ⁱ Pr H H F OH XXVIII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H H F OH XXVIII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVTII-29-8 p-Br-Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-30-1 p-i-ph H H H ⁱ Pr H H F OH XXVIII-30-2 p-i-ph H H CH ₃ ⁱ Pr H H F OH XXVIII-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXVIII-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H H F OH XXVIII-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXVIII-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXVIII-30-8 p-i-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-31-1 CH ₃ N n n ⁿ Bu H H F OH XXVIII-31-2 CH ₃ N n CH ₃ ⁿ Bu H H F OH XXVIII-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H H F OH XXVTII-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-31-8 CH ₃ * n * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-32-1 Et H H H ⁿ Bu H H F OH XXVIII-32-2 Et H H CH ₃ ⁿ Bu H H F OH XXVIII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-32-5 Et H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-32-8 Et * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-33-1 ⁱ Pr H H H ⁿ Bu H H F OH XXVIII-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H H F OH XXVIII-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-33-8 ⁱ Pr * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-34-1 ^t Bu H H H ⁿ Bu H H F OH XXVIII-34-2 ^t Bu H H CH ₃ ⁿ Bu H H F OH XXVIII-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-34-8 ^t Bu * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-35-1 Ph H H H ⁿ Bu H H F OH XXVIII-35-2 Ph H H CH ₃ ⁿ Bu H H F OH XXVIII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-35-5 Ph H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-35-8 Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-36-1 p-me-ph H H H ⁿ Bu H H F OH XXVIII-36-2 p-me-ph H H CH ₃ ⁿ Bu H H F OH XXVIII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-36-8 p-me-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-37-1 p-f-ph H H H ⁿ Bu H H F OH XXVIII-37-2 p-f-ph H H CH ₃ ⁿ Bu H H F OH XXVIII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-37-8 p-f-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-38-1 p-Cl-Ph H H H ⁿ Bu H H F OH XXVIII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H H F OH XXVIII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-38-8 p-Cl-Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-39-1 p-Br-Ph H H H ⁿ Bu H H F OH XXVIII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H H F OH XXVIII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-39-8 p-Br-Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-40-1 p-i-ph H H H ⁿ Bu H H F OH XXVIII-40-2 p-i-ph H H CH ₃ ⁿ Bu H H F OH XXVIII-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXVIII-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H H F OH XXVIII-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXVIII-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXVIII-40-8 p-i-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-41-1 CH ₃ N N n Bz H H F OH XXVIII-41-2 CH ₃ N N CH ₃ Bz H H F OH XXVIII-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H H F OH XXVIII-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-41-5 CH ₃ N n CH ₂ Ph Bz H H F OH XXVIII-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H H F OH XXVIII-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-41-8 CH ₃ * n * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-42-1 Et H H H Bz H H F OH XXVIII-42-2 Et H H CH ₃ Bz H H F OH XXVIII-42-3 Et H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-42-5 Et H H CH ₂ Ph Bz H H F OH XXVIII-42-6 Et H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-42-8 Et * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-43. No. R R Rja Rjb R R R X Y XXVIII-43-1 ⁱ Pr H H H Bz H H F OH XXVIII-43-2 ⁱ Pr H H CH ₃ Bz H H F OH XXVIII-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-43-5 ⁱ Pr H H CH ₂ Ph Bz H H F OH XXVIII-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-43-8 ⁱ Pr * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-44-1 ^t Bu H H H Bz H H F OH XXVIII-44-2 ^t Bu H H CH ₃ Bz H H F OH XXVIII-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-44-5 ^t Bu H H CH ₂ Ph Bz H H F OH XXVIII-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-44-8 ^t Bu * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-45-1 Ph H H H Bz H H F OH XXVIII-45-2 Ph H H CH ₃ Bz H H F OH XXVIII-45-3 Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVHI-45-5 Ph H H CH ₂ Ph Bz H H F OH XXVIII-45-6 Ph H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-45-8 Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-46-1 p-me-ph H H H Bz H H F OH XXVIII-46-2 p-me-ph H H CH ₃ Bz H H F OH XXVIII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-46-5 p-me-ph H H CH ₂ Ph Bz H H F OH XXVIII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-46-8 p-me-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-47-1 p-f-ph H H H Bz H H F OH XXVIII-47-2 p-f-ph H H CH ₃ Bz H H F OH XXVIII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-47-5 p-f-ph H H CH ₂ Ph Bz H H F OH XXVIII-47-b p-f-ph H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-47-8 p-f-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-48-1 p-Cl-Ph H H H Bz H H F OH XXVIII-48-2 p-Cl-Ph H H CH ₃ Bz H H F OH XXVIII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H H F OH XXVIII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-48-8 p-Cl-Ph * H * Bz H H F OH> * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXVIII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-49-1 p-Br-Ph H H H Bz H H F OH XXVIII-49-2 p-Br-Ph H H CH ₃ Bz H H F OH XXVIII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-49-5 p-Br-Ph H H CH ₂ Ph Bz H H F OH XXVIII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-49-8 p-Br-Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXVIII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXVIII-50-1 p-i-ph H H H Bz H H F OH XXVIII-50-2 p-i-ph H H CH ₃ Bz H H F OH XXVIII-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXVIII-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXVIII-50-5 p-i-ph H H CH ₂ Ph Bz H H F OH XXVIII-50-b p-i-ph H H CH ₂ -indol-3-yl Bz H H F OH XXVIII-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXVIII-50-8 p-i-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-1-1 CH ₃ N n n CH ₃ N CH ₃ F IT XXIX-1-2 CH ₃ N n CH ₃ CH ₃ N CH ₃ F IT XXIX-1-3 CH ₃ N n CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-1-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-1-5 CH ₃ N n CH ₂ Ph CH ₃ n CH ₃ F IT XXIX-1-6 CH ₃ N n CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXIX-1-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXIX-1-8 CH ₃ * n * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-2-1 Et H H H CH ₃ H CH ₃ F OH XXIX-2-2 Et H H CH ₃ CH ₃ H CH ₃ F OH XXIX-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXIX-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXIX-2-5 Et H H CH ₂ Ph CH ₃ H CH ₃ F OH XXIX-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXIX-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXIX-2-8 Et * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-3. No. R R R3b R R R X Y XXIX-3-1 ⁱ Pr H H H CH ₃ H CH ₃ F OH XXIX-3-2 ⁱ Pr H H CH ₃ CH ₃ H CH ₃ F OH XXIX-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXIX-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXIX-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ H CH ₃ F OH XXIX-3-6 ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXIX-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXIX-3-8 ⁱ Pr * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-4. No. R R Rja R3b R R * R X Y XXIX-4-1 ^t Bu H H H CH ₃ H CH ₃ F OH XXIX-4-2 ^t Bu H H CH ₃ CH ₃ H CH ₃ F OH XXIX-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXIX-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H CH ₃ F OH XXIX-4-5 ^t Bu H H CH ₂ Ph CH ₃ H CH ₃ F OH XXIX-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ H CH ₃ F OH XXIX-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ H CH ₃ F OH XXIX-4-8 ^t Bu * H * CH ₃ H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-5-1 Ph H H H CH ₃ N CH ₃ F IT XXIX-5-2 Ph H H CH ₃ CH ₃ n CH ₃ F IT XXIX-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-5-5 Ph H H CH ₂ Ph CH ₃ n CH ₃ F IT XXIX-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXIX-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXIX-5-8 Ph * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-6-1 p-me-ph H H H CH ₃ N CH ₃ F IT XXIX-6-2 p-me-ph H H CH ₃ CH ₃ N CH ₃ F IT XXIX-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXIX-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXIX-6-5 p-me-ph H H CH ₂ Ph CH ₃ N CH ₃ F IT XXIX-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXIX-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT XXIX-6-8 p-me-ph * H * CH ₃ N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-7-1 p-f-ph H H H CH ₃ N CH ₃ F IT XXIX-7-2 p-f-ph H H CH ₃ CH ₃ n CH ₃ F IT XXIX-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-7-6 p-f-ph H H CH ₂ Ph CH ₃ n CH ₃ F IT XXIX-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXIX-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXIX-7-20 p-f-ph * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-8-1 p-Cl-Ph H H H CH ₃ N CH ₃ F IT XXIX-8-2 p-Cl-Ph H H CH ₃ CH ₃ N CH ₃ F IT XXIX-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXIX-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXIX-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N CH ₃ F IT XXIX-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N CH ₃ F IT XXIX-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N CH ₃ F IT XXIX-8-8 p-Cl-Ph * H * CH ₃ N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-9-1 p-Br-Ph H H H CH ₃ n CH ₃ F IT XXIX-9-2 p-Br-Ph H H CH ₃ CH ₃ n CH ₃ F IT XXIX-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ n CH ₃ F IT XXIX-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXIX-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXIX-9-20 p-Br-Ph * H * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-10-1 p-1-ph N N n CH ₃ N CH ₃ F IT XXIX-10-2 p-1-ph N N CH ₃ CH ₃ N CH ₃ F IT XXIX-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N CH ₃ F IT XXIX-10-4 p-1-ph N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n CH ₃ F IT XXIX-10-5 p-1-ph N N CH ₂ Ph CH ₃ n CH ₃ F IT XXIX-10-6 p-1-ph N N CH ₂ -indol-3-yl CH ₃ n CH ₃ F IT XXIX-10-7 p-1-ph N N CH ₂ CH ₂ SCH ₃ CH ₃ n CH ₃ F IT XXIX-10-8 p-1-ph * N * CH ₃ n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-11-1 CH ₃ N N n Et H CH ₃ F IT XXIX-11-2 CH ₃ N N CH ₃ Et H CH ₃ F IT XXIX-11-3 CH ₃ N N CH (CH ₃ ) ₂ Et H CH ₃ F it XXIX-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F it XXIX-11-5 CH ₃ N n CH ₂ Ph Et H CH ₃ F it XXIX-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H CH ₃ F it XXIX-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F it XXIX-11-8 CH ₃ * n * Et H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-12-1 Et H H H Et H CH ₃ F IT XXIX-12-2 Et H H CH ₃ Et H CH ₃ F IT XXIX-12-3 Et H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-12-5 Et H H CH ₂ Ph Et H CH ₃ F IT XXIX-12-6 Et H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXIX-12-8 Et * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-13-1 ⁱ Pr N N n Et H CH ₃ F IT XXIX-13-2 ⁱ Pr N N CH ₃ Et H CH ₃ F IT XXIX-13-3 ⁱ Pr N N CH (CH ₃ ) ₂ Et H CH ₃ F it XXIX-13-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F it XXIX-13-5 ⁱ Pr N n CH ₂ Ph Et H CH ₃ F it XXIX-13-6 ⁱ Pr N n CH ₂ -indol-3-yl Et H CH ₃ F it XXIX-13-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Et H CH ₃ F it XXIX-13-8 ⁱ Pr * n * Et H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-14-1 ^t Bu H H H Et H CH ₃ F IT XXIX-14-2 ^t Bu H H CH ₃ Et H CH ₃ F IT XXIX-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) Et H CH ₃ F IT XXIX-14-5 ^t Bu H H CH ₂ Ph Et H CH ₃ F IT XXIX-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-14-7 ^t Bu H H CH ₂ CH ₂ SCH Et H CH ₃ F IT XXIX-14-8 ^t Bu * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXX-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-15-1 Ph H H H Et H CH ₃ F IT XXIX-15-2 Ph H H CH ₃ Et H CH ₃ F IT XXIX-15-3 Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-15-5 Ph H H CH ₂ Ph Et H CH ₃ F IT XXIX-15-6 Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F it XXIX-15-8 Ph * H * Et H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-16-1 p-me-ph H H H Et H CH ₃ F IT XXIX-16-2 p-me-ph H H CH ₃ Et H CH ₃ F IT XXIX-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-16-5 p-me-ph H H CH ₂ Ph Et H CH ₃ F IT XXIX-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-16-8 p-me-ph * H * Et H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-17-1 p-f-ph H H H Et H CH ₃ F IT XXIX-17-2 p-f-ph H H CH ₃ Et H CH ₃ F IT XXIX-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-17-4 p-f-ph H n CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-17-5 p-f-ph H H CH ₂ Ph Et H CH ₃ F IT XXIX-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXIX-17-8 p-f-ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-18-1 p-Cl-Ph H H H Et H CH ₃ F IT XXIX-18-2 p-Cl-Ph H H CH ₃ Et H CH ₃ F IT XXIX-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-18-5 p-Cl-Ph H H Chzph Et H CH ₃ F IT XXIX-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXIX-18-8 p-Cl-Ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-19-1 p-Br-Ph H H H Et H CH ₃ F IT XXIX-19-2 p-Br-Ph H H CH ₃ Et H CH ₃ F IT XXIX-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-19-5 p-Br-Ph H H CH ₂ Ph Et H CH ₃ F IT XXIX-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F OH XXIX-19-8 p-Br-Ph * H * Et H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-20-1 p-i-ph H H H Et H CH ₃ F IT XXIX-20-2 p-i-ph H H CH ₃ Et H CH ₃ F IT XXIX-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H CH ₃ F IT XXIX-20-5 p-i-ph H H CH ₂ Ph Et H CH ₃ F IT XXIX-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H CH ₃ F IT XXIX-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H CH ₃ F IT XXIX-20-8 p-i-ph * H * Et H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-21-1 CH ₃ N N N ⁱ Pr N CH ₃ F IT XXIX-21-2 CH ₃ N N CH ₃ ⁱ Pr N CH ₃ F IT XXIX-21-3 CH ₃ N N CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXIX-21-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N CH ₃ F IT XXIX-21-5 CH ₃ N N CH ₂ Ph ⁱ Pr N CH ₃ F IT XXIX-21-6 CH ₃ N N CH ₂ -indol-3-yl ⁱ Pr N CH ₃ F IT XXIX-21-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁱ Pr N CH ₃ F IT XXIX-21-8 CH ₃ * N * ⁱ Pr N CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-22-1 Et H H H ⁱ Pr H CH ₃ F IT XXIX-22-2 Et H H CH ₃ ⁱ Pr H CH ₃ F IT XXIX-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-22-5 Et H H CH ₂ Ph ⁱ Pr H CH ₃ F IT

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXIX-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXIX-22-8 Et * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-23-1 ⁱ Pr H H H ⁱ Pr H CH ₃ F IT XXIX-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H CH ₃ F IT XXIX-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXIX-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXIX-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXIX-23-8 ⁱ Pr * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-24-1 ^t Bu N N N ⁱ Pr N CH ₃ F IT XXIX-24-2 ^t Bu N N CH ₃ ⁱ Pr N CH ₃ F IT XXIX-24-3 ^t Bu N N CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXIX-24-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT XXIX-24-5 ^t Bu N N CH ₂ Ph ⁱ Pr n CH ₃ F IT XXIX-24-6 ^t Bu N N CH ₂ -indol-3-yl ⁱ Pr n CH ₃ F IT XXIX-24-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ ⁱ Pr n CH ₃ F IT XXIX-24-8 ^t Bu N * ⁱ Pr n CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-25-1 Ph H H H ⁱ Pr H CH ₃ F OH XXIX-25-2 Ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXIX-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXIX-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-25-5 Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXIX-25-6 Ph H H CHg-indol-3-yl ⁱ Pr H CH ₃ F OH XXIX-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXIX-25-8 Ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-26-1 p-me-ph H H H ⁱ Pr H CH ₃ F IT XXIX-26-2 p-me-ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXIX-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F it XXIX-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F it XXIX-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F it XXIX-26-8 p-me-ph * H * ⁱ Pr H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-27-1 p-f-ph H H H ⁱ Pr H CH ₃ F IT XXIX-27-2 p-f-ph H H CH ₃ ⁱ Pr H CH ₃ F IT XXIX-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F IT XXIX-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F IT XXIX-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F IT XXIX-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F IT XXIX-27-8 p-f-ph * H * ⁱ Pr H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXX-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y HHGH-28-1 p-Cl-Ph H n n ⁱ Pr N CH ₃ F IT XXIX-28-2 p-Cl-Ph H n CH ₃ ⁱ Pr N CH ₃ F IT XXIX-28-3 p-Cl-Ph N n CH (CH ₃ ) ₂ ⁱ Pr n CH ₃ F IT

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXIX-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXIX-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXIX-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXIX-28-8 p-Cl-Ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-29-1 p-Br-Ph H H H ⁱ Pr H CH ₃ F OH XXIX-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXIX-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXIX-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXIX-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXIX-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXIX-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXIX-29-8 p-Br-Ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-30-1 p-i-ph H H H ⁱ Pr H CH ₃ F OH XXIX-30-2 p-i-ph H H CH ₃ ⁱ Pr H CH ₃ F OH XXIX-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXIX-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H CH ₃ F OH XXIX-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H CH ₃ F OH XXIX-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H CH ₃ F OH XXIX-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H CH ₃ F OH XXIX-30-8 p-i-ph * H * ⁱ Pr H CH ₃ F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-31-1 CH ₃ H H H ⁿ Bu H CH ₃ F OH XXIX-31-2 CH ₃ H H CH ₃ ⁿ Bu H CH ₃ F OH

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-31-8 CH ₃ * n * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-32-1 Et H H H ⁿ Bu H CH ₃ F IT XXIX-32-2 Et H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-32-5 Et H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-32-8 Et * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-33-1 ⁱ Pr n N n ⁿ Bu H CH ₃ F IT XXIX-33-2 ⁱ Pr n N CH ₃ ⁿ Bu H CH ₃ F IT XXIX-33-3 ⁱ Pr N N CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-33-4 ⁱ Pr n N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-33-5 ⁱ Pr n N CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-33-6 ⁱ Pr N n CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-33-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-33-8 ⁱ Pr * n * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-34-1 ^t Bu N N N ⁿ Bu N CH ₃ F IT

No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-34-2 ^t Bu H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-34-8 ^t Bu * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-35-1 Ph H H H ⁿ Bu H CH ₃ F IT XXIX-35-2 Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-35-5 Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-35-8 Ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-36-1 p-me-ph H H H ⁿ Bu H CH ₃ F IT XXIX-36-2 p-me-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-36-6 p-me-ph H H CHg-indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-36-8 p-me-ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-37-1 p-f-ph H H H ⁿ Bu H CH ₃ F IT XXIX-37-2 p-f-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-37-8 p-f-ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-38-1 p-Cl-Ph H H H ⁿ Bu H CH ₃ F IT XXIX-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-38-8 p-Cl-Ph H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-39-1 p-Br-Ph H H H ⁿ Bu H CH ₃ F IT XXIX-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-39-8 p-Br-Ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-40-1 p-i-ph H H H ⁿ Bu H CH ₃ F IT XXIX-40-2 p-i-ph H H CH ₃ ⁿ Bu H CH ₃ F IT XXIX-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H CH ₃ F IT XXIX-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H CH ₃ F IT XXIX-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H CH ₃ F IT XXIX-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H CH ₃ F IT XXIX-40-8 p-i-ph * H * ⁿ Bu H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-41-1 CH ₃ N N n Bz H CH ₃ F IT XXIX-41-2 CH ₃ N N CH ₃ Bz H CH ₃ F IT XXIX-41-3 CH ₃ N n CH (CH ₃ ) ₂ Bz H CH ₃ F XXIX-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-41-5 CH ₃ N n CH ₂ Ph Bz H CH ₃ F it XXIX-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H CH ₃ F it XXIX-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F it XXIX-41-8 CH ₃ * n * Bz H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-42-1 Et H H H Bz H CH ₃ F IT XXIX-42-2 Et H H CH ₃ Bz H CH ₃ F IT XXIX-42-3 Et H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-42-5 Et H H CH ₂ Ph Bz H CH ₃ F IT XXIX-42-6 Et H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-42-8 Et * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-43-1 ⁱ Pr N N n Bz H CH ₃ F IT XXIX-43-2 ⁱ Pr N N CH ₃ Bz H CH ₃ F IT XXIX-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-43-4 ⁱ Pr N N CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-43-5 ⁱ Pr N N CH ₂ Ph Bz H CH ₃ F IT XXIX-43-6 ⁱ Pr N N CH ₂ -indol-3-yl Bz H CH ₃ F IT HHHH-43-7 ⁱ Pr N N CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-43-8 ⁱ Pr * N * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-44-1 ^t Bu N N n Bz H CH ₃ F IT XXIX-44-2 ^t Bu N n CH ₃ Bz H CH ₃ F IT XXIX-44-3 ^t Bu N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-44-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-44-5 ^t Bu n n CH ₂ Ph Bz H CH ₃ F IT XXIX-44-6 ^t Bu n n CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-44-7 ^t Bu n n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-44-8 ^t Bu * n * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-45-1 Ph H H H Bz H CH ₃ F IT XXIX-45-2 Ph H H CH ₃ Bz H CH ₃ F IT XXIX-45-3 Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F it XXIX-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F it XXIX-45-5 Ph H H CH ₂ Ph Bz H CH ₃ F it XXIX-45-6 Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F it XXIX-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F it XXIX-45-8 Ph * H * Bz H CH ₃ F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-46-1 p-me-ph H H H Bz H CH ₃ F IT XXIX-46-2 p-me-ph H H CH ₃ Bz H CH ₃ F IT XXIX-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-46-5 p-me-ph H H CH ₂ Ph Bz H CH ₃ F IT XXIX-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-46-8 p-me-ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-47-1 p-f-ph H H H Bz H CH ₃ F IT XXIX-47-2 p-f-ph H H CH ₃ Bz H CH ₃ F IT XXIX-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-47-5 p-f-ph H H CH ₂ Ph Bz H CH ₃ F IT XXIX-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-47-8 p-f-ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-48-1 p-Cl-Ph H H H Bz H CH ₃ F IT XXIX-48-2 p-Cl-Ph H H CH ₃ Bz H CH ₃ F IT XXIX-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-48-5 p-Cl-Ph H H CH ₂ Ph Bz H CH ₃ F IT XXIX-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-48-8 p-Cl-Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXIX-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-49-1 p-Br-Ph H H H Bz H CH ₃ F IT XXIX-49-2 p-Br-Ph H H CH ₃ Bz H CH ₃ F IT XXIX-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-49-5 p-Br-Ph H H CH ₂ Ph Bz H CH ₃ F IT XXIX-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-49-8 p-Br-Ph * H * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXIX-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXIX-50-1 p-1-ph N n n Bz H CH ₃ F IT XXIX-50-2 p-1-ph N n CH ₃ Bz H CH ₃ F IT XXIX-50-3 p-1-ph N n CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-50-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ Bz H CH ₃ F IT XXIX-50-5 p-1-ph N n CH ₂ Ph Bz H CH ₃ F IT XXIX-50-6 p-1-ph N n CH ₂ -indol-3-yl Bz H CH ₃ F IT XXIX-50-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ Bz H CH ₃ F IT XXIX-50-8 p-1-ph * n * Bz H CH ₃ F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-1-1 CH ₃ N n n CH ₃ N F N IT XXX-1-2 CH ₃ N n CH ₃ CH ₃ N F N IT XXX-1-3 CH ₃ n n CH (CH ₃ ) ₂ CH ₃ N F N IT XXX-1-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n IT Xxx-1-5 CH ₃ n n CH ₂ Ph CH ₃ N F n it XXX-1-6 CH ₃ n n CH ₂ -indol-3-yl CH ₃ N F n it XXX-1-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ CH ₃ N F n it XXX-1-8 CH ₃ * n * CH ₃ N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-2-1 Et H H H CH ₃ H F n IT Xxx-2-2 Et H H CH ₃ CH ₃ H F n IT XXX-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N F n it Xxx-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F n it Xxx-2-5 Et H H CH ₂ Ph CH ₃ N F n it Xxx-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N F n it Xxx-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N F n it Xxx-2-8 Et * H * CH ₃ N F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-3-1 ⁱ Pr n n n CH ₃ N F N IT Xxx-3-2 ⁱ Pr n n CH ₃ CH ₃ N F N IT xxx-3-3 ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ n F N IT XXX-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ n F N IT XXX-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ n F N IT XXX-3-6 ⁱ Pr n n CH ₂ -indol-3-yl CH ₃ n F N IT Xxx-3-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ CH ₃ n F N IT Xxx-3-8 ⁱ Pr * n * CH ₃ n F N it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-4-1 ^t Bu N N n CH ₃ N F n IT XXX-4-2 ^t Bu N N CH ₃ CH ₃ n F n IT Xxx-4-3 ^t Bu N N CH (CH ₃ ) ₂ CH ₃ n F n it XXX-4-4 ^t Bu N N CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it Xxx-4-5 ^t Bu N N CH ₂ Ph CH ₃ n F n it XXX-4-6 ^t Bu N N CH ₂ -indol-3-yl CH ₃ n F n it Xxx-4-7 ^t Bu N N CH ₂ CH ₂ SCH ₃ CH ₃ n F n it Xxx-4-8 ^t Bu * n * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-5-1 Ph H H H CH ₃ N F n IT XXX-5-2 Ph H H CH ₃ CH ₃ N F n IT Xxx-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n F n it XXX-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it Xxx-5-5 Ph H H CH ₂ Ph CH ₃ n F n it XXX-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n F n it Xxx-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it Xxx-5-8 Ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-6-1 p-me-ph H H H CH ₃ N F N it Xxx-6-2 p-me-ph H H CH ₃ CH ₃ N F N it Xxx-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N F N IT XXX-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT Xxx-6-5 p-me-ph H H CH ₂ Ph CH ₃ N F N IT XXX-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N F N IT Xxx-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT Xxx-6-8 p-me-ph H * CH ₃ N F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-7-1 p-f-ph H H H CH ₃ N F n IT XXX-7-2 p-f-ph H H CH ₃ CH ₃ n F n IT XXX-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n F n it Xxx-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F n it XXX-7-6 p-f-ph H H CH ₂ Ph CH ₃ n F n it Xxx-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n F n it Xxx-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F n it XXX-7-20 p-f-ph * H * CH ₃ n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-8-1 p-Cl-Ph H H H CH ₃ N F N IT XXX-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F N IT XXX-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N F N IT XXX-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT Xxx-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N F N IT XXX-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N F N IT Xxx-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT Xxx-8-8 p-Cl-Ph * H * CH ₃ N F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-9-1 p-Br-Ph H H H CH ₃ N F N IT XXX-9-2 p-Br-Ph H H CH ₃ CH ₃ N F N IT XXX-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F N IT XXX-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N IT XXX-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F N IT XXX-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N F N IT XXX-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F N IT XXX-9-20 p-Br-Ph * H * CH ₃ N F N IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-10-1 p-1-ph N n n CH ₃ N F N IT XXX-10-2 p-1-ph N n CH ₃ CH ₃ N F N IT XXX-10-3 p-1-ph n n CH (CH ₃ ) ₂ CH ₃ N F N it XXX-10-4 p-1-ph n n CH ₂ CH (CH ₃ ) ₂ CH ₃ N F N it Xxx-10-5 p-1-ph n n CH ₂ Ph CH ₃ N F N it XXX-10-6 p-1-ph n n CH ₂ -indol-3-yl CH ₃ N F N it Xxx-10-7 p-1-ph n n CH ₂ CH ₂ SCH ₃ CH ₃ n F N it Xxx-10-8 p-1-ph * n * CH ₃ n F N it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-11-1 CH ₃ N n n Et H F H OH Xxx-11-2 CH ₃ N n CH ₃ Et H F H OH Xxx-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H F H OH Xxx-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-11-5 CH ₃ N n CH ₂ Ph Et H F H OH XXX-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H F H OH XXX-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H F H OH XXX-11-8 CH ₃ * n * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-12-1 Et H H H Et H F H OH Xxx-12-2 Et H H CH ₃ Et H F H OH Xxx-12-3 Et H H CH (CH ₃ ) ₂ Et H F H OH Xxx-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-12-5 Et H H CH ₂ Ph Et H F H OH XXX-12-6 Et H H CH ₂ -indol-3-yl Et H F H OH XXX-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F H OH Xxx-12-8 Et * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-13-1 ⁱ Pr N n n Et H F H OH XXX-13-2 ⁱ Pr N n CH ₃ Et H F H OH XXX-13-3 ⁱ Pr n n CH (CH ₃ ) ₂ Et H F H OH XXX-13-4 ⁱ Pr n n CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-13-5 ⁱ Pr n n CH ₂ Ph Et H F H OH XXX-13-6 ⁱ Pr n n CH ₂ -indol-3-yl Et H F H OH XXX-13-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ Et H F H OH XXX-13-8 ⁱ Pr * n * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-14-1 ^t Bu H H H Et H F H OH Xxx-14-2 ^t Bu H H CH ₃ Et H F H OH Xxx-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H F H OH Xxx-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-14-5 ^t Bu H H CH ₂ Ph Et H F H OH XXX-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H F H OH Xxx-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H F H OH Xxx-14-8 ^t Bu * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-15-1 Ph H H H Et H F H OH Xxx-15-2 Ph H H CH ₃ Et H F H OH XXX-15-3 Ph H H CH (CH ₃ ) ₂ Et H F H OH Xxx-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-15-5 Ph H H CH ₂ Ph Et H F H OH XXX-15-6 Ph H H CH ₂ -indol-3-yl Et H F H OH XXX-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH Xxx-15-8 Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-16-1 p-me-ph H H H Et H F H OH XXX-16-2 p-me-ph H H CH ₃ Et H F H OH XXX-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F H OH XXX-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXX-16-5 p-me-ph H H CH ₂ Ph Et H F H OH XXX-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F H OH XXX-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXX-16-8 p-me-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-17-1 p-f-ph H H H Et H F H OH XXX-17-2 p-f-ph H H CH ₃ Et H F H OH XXX-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F H OH XXX-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH XXX-17-5 p-f-ph H H CH ₂ Ph Et H F H OH XXX-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F H OH XXX-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXX-17-8 p-f-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-18-1 p-Cl-Ph H H H Et H F H OH Xxx-18-2 p-Cl-Ph H H CH ₃ Et H F H OH Xxx-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F H OH Xxx-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-18-5 p-Cl-Ph H H CH ₂ Ph Et H F H OH XXX-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F H OH XXX-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXX-18-8 p-Cl-Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-19-1 p-Br-Ph H H H Et H F H OH XXX-19-2 p-Br-Ph H H CH ₃ Et H F H OH XXX-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F H OH XXX-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-19-5 p-Br-Ph H H CH ₂ Ph Et H F H OH XXX-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F H OH XXX-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH XXX-19-8 p-Br-Ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-20-1 p-i-ph H H H Et H F H OH Xxx-20-2 p-i-ph H H CH ₃ Et H F H OH Xxx-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H F H OH Xxx-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F H OH Xxx-20-5 p-i-ph H H CH ₂ Ph Et H F H OH XXX-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H F H OH XXX-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H F H OH Xxx-20-8 p-i-ph * H * Et H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-21-1 CH ₃ N n n ⁱ Pr N F n IT XXX-21-2 CH ₃ N n CH ₃ ⁱ Pr N F n IT XXX-21-3 CH ₃ n n CH (CH ₃ ) ₂ ⁱ Pr n F n it XXX-21-4 CH ₃ n n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr n F n it XXX-21-5 CH ₃ n n CH ₂ Ph ⁱ Pr n F n it XXX-21-6 CH ₃ n n CH ₂ -indol-3-yl ⁱ Pr n F n it XXX-21-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁱ Pr n F n it XXX-21-8 CH ₃ * n * ⁱ Pr n F n it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-22-1 Et H H H ⁱ Pr H F H OH XXX-22-2 Et H H CH ₃ ⁱ Pr H F H OH XXX-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-22-5 Et H H CH ₂ Ph * Pr H F H OH XXX-22-6 Et H H CH ₂ -indol-3-yl * Pr H F H OH XXX-22-7 Et H H CH ₂ CH ₂ SCH ₃ * Pr H F H OH XXX-22-8 Et * H * * Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-23-1 ⁱ Pr H H H ⁱ Pr H F H OH XXX-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H F H OH Xxx-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ * Pr H F H OH XXX-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ * Pr H F H OH XXX-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H F H OH XXX-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-23-8 ⁱ Pr * H * * Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-24-1 ^t Bu H H H ⁱ Pr H F H OH XXX-24-2 ^t Bu H H CH ₃ ⁱ Pr H F H OH XXX-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H F H OH XXX-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-24-8 ^t Bu * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-25-1 Ph H H H ⁱ Pr H F H OH XXX-25-2 Ph H H CH ₃ ⁱ Pr H F H OH XXX-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-25-5 Ph H H CH ₂ Ph ⁱ Pr H F H OH XXX-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-25-8 Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-26-1 p-me-ph H H H ⁱ Pr H F H OH XXX-26-2 p-me-ph H H CH ₃ ⁱ Pr H F H OH XXX-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F H OH XXX-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-26-8 p-me-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-27-1 p-f-ph H H H ⁱ Pr H F H OH XXX-27-2 p-f-ph H H CH ₃ ⁱ Pr H F H OH XXX-27-3 p-f-ph H H CH (CH ₃ ) ₂ tr H F H OH XXX-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F H OH XXX-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-27-8 p-f-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-28-1 p-Cl-Ph H H H ⁱ Pr H F H OH XXX-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F H OH XXX-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F H OH XXX-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-28-8 p-Cl-Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-29-1 p-Br-Ph H H H ⁱ Pr H F H OH XXX-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F H OH XXX-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F H OH XXX-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-29-8 p-Br-Ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-30-1 p-i-ph H H H ⁱ Pr H F H OH XXX-30-2 p-i-ph H H CH ₃ ⁱ Pr H F H OH XXX-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F H OH XXX-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H F H OH XXX-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H F H OH XXX-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F H OH XXX-30-8 p-i-ph * H * ⁱ Pr H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-31-1 CH ₃ N N n ⁿ Bu H F H OH XXX-31-2 CH ₃ N N CH ₃ ⁿ Bu H F H OH XXX-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-31-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-31-5 CH ₃ N N CH ₂ Ph ⁿ Bu H F H OH XXX-31-6 CH ₃ N N CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-31-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-31-8 CH ₃ * N * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-32-1 Et H H H ⁿ Bu H F H OH Xxx-32-2 Et H H CH ₃ ⁿ Bu H F H OH Xxx-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH Xxx-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-32-5 Et H H CH ₂ Ph ⁿ Bu H F H OH XXX-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-32-8 Et * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-33-1 ⁱ Pr H H H ⁿ Bu H F H OH Xxx-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H F H OH XXX-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H F H OH XXX-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-33-8 ⁱ Pr * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-34-1 ^t Bu N n n ⁿ Bu N F N IT XXX-34-2 ^t Bu N n CH ₃ ⁿ Bu N F N IT Xxx-34-3 ^t Bu N n CH (CH ₃ ) ₂ ⁿ Bu N F N IT XXX-34-4 ^t Bu N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu N F N IT Xxx-34-5 ^t Bu N n CH ₂ Ph ⁿ Bu N F N IT XXX-34-6 ^t Bu N n CH ₂ -indol-3-yl ⁿ Bu N F N it XXX-34-7 ^t Bu N n CH ₂ CH ₂ SCH ₃ ⁿ Bu N F N it XXX-34-8 ^t Bu * n * ⁿ Bu N F N it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-35-1 Ph H H H ⁿ Bu H F H OH XXX-35-2 Ph H H CH ₃ ⁿ Bu H F H OH XXX-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH Xxx-35-5 Ph H H CH ₂ Ph ⁿ Bu H F H OH XXX-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH Xxx-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-35-8 Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-36-1 p-me-ph H H H ⁿ Bu H F H OH Xxx-36-2 p-me-ph H H CH ₃ ⁿ Bu H F H OH XXX-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH Xxx-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F H OH XXX-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-36-8 p-me-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-37-1 p-f-ph H H H ⁿ Bu H F H OH XXX-37-2 p-f-ph H H CH ₃ ⁿ Bu H F H OH XXX-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F H OH XXX-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-37-8 p-f-ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-38-1 p-Cl-Ph H H H ⁿ Bu H F H OH XXX-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F H OH Xxx-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F H OH XXX-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-38-8 p-Cl-Ph * H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-39-1 p-Br-Ph H H H ⁿ Bu H F H OH XXX-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F H OH XXX-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F H OH XXX-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-39-8 p-Br-Ph H * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-40-1 p-1-ph N n N ⁿ Bu H F H OH XXX-40-2 p-1-ph N n CH ₃ ⁿ Bu H F H OH XXX-40-3 p-1-ph N n CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-40-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F H OH XXX-40-5 p-1-ph N n CH ₂ Ph ⁿ Bu H F H OH XXX-40-6 p-1-ph N n CH ₂ -indol-3-yl ⁿ Bu H F H OH XXX-40-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F H OH XXX-40-8 p-1-ph * n * ⁿ Bu H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-41-1 CH ₃ N N n Bz H F H OH XXX-41-2 CH ₃ N N CH ₃ Bz H F H OH XXX-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H F H OH XXX-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-41-5 CH ₃ N n CH ₂ Ph Bz H F H OH XXX-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H F H OH XXX-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-41-8 CH ₃ * n * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-42-1 Et H H H Bz H F H OH Xxx-42-2 Et H H CH ₃ Bz H F H OH XXX-42-3 Et H H CH (CH ₃ ) ₂ Bz H F H OH Xxx-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-42-5 Et H H CH ₂ Ph Bz H F H OH XXX-42-6 Et H H CH ₂ -indol-3-yl Bz H F H OH XXX-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-42-8 Et * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-43-1 ⁱ Pr N N n Bz H F H OH XXX-43-2 ⁱ Pr N N CH ₃ Bz H F H OH XXX-43-3 ⁱ Pr N N CH (CH ₃ ) ₂ Bz H F H OH XXX-43-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ Bz H F H OH Xxx-43-5 ⁱ Pr N n CH ₂ Ph Bz H F H OH XXX-43-6 ⁱ Pr N n CH ₂ -indol-3-yl Bz H F H OH XXX-43-7 ⁱ Pr N n CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-43-8 ⁱ Pr * n * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-44-1 ^t Bu H H H Bz H F H OH Xxx-44-2 ^t Bu H H CH ₃ Bz H F H OH Xxx-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H F H OH XXX-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-44-5 ^t Bu H H CH ₂ Ph Bz H F H OH XXX-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H F H OH XXX-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-44-8 ^t Bu * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-45-1 Ph H H H Bz H F H OH XXX-45-2 Ph H H CH ₃ Bz H F H OH XXX-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXX-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-45-5 Ph H H CH ₂ Ph Bz H F H OH XXX-45-6 Ph H H CH ₂ -indol-3-yl Bz H F H OH XXX-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-45-8 Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-46-1 p-me-ph H H H Bz H F H OH XXX-46-2 p-me-ph H H CH ₃ Bz H F H OH XXX-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXX-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-46-5 p-me-ph H H CH ₂ Ph Bz H F H OH XXX-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F H OH XXX-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-46-8 p-me-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-47-1 p-f-ph H H H Bz H F H OH Xxx-47-2 p-f-ph H H CH ₃ Bz H F H OH XXX-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F H OH Xxx-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-47-5 p-f-ph H H CH ₂ Ph Bz H F H OH XXX-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F H OH XXX-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH Xxx-47-8 p-f-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-48-1 p-Cl-Ph H H H Bz H F H OH Xxx-48-2 p-Cl-Ph H H CH ₃ Bz H F H OH XXX-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F H OH Xxx-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH XXX-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F H OH XXX-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F H OH XXX-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-48-8 p-Cl-Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXX-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXX-49-1 p-Br-Ph H H H Bz H F H OH XXX-49-2 p-Br-Ph H H CH ₃ Bz H F H OH XXX-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F H OH XXX-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH Xxx-49-5 p-Br-Ph H H CH ₂ Ph Bz H F H OH XXX-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H F H OH XXX-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-49-8 p-Br-Ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXX-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxx-50-1 p-i-ph H H H Bz H F H OH Xxx-50-2 p-i-ph H H CH ₃ Bz H F H OH XXX-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H F H OH XXX-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F H OH Xxx-50-5 p-i-ph H H CH ₂ Ph Bz H F H OH XXX-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H F H OH XXX-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H F H OH XXX-50-8 p-i-ph * H * Bz H F H OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-1-1 CH ₃ H H H CH ₃ H F F OH XXXI-1-2 CH ₃ H H CH ₃ CH ₃ H F F OH XXXI-1-3 CH ₃ H H CH (CH ₃ ) ₂ CH ₃ H F F OH XXXI-1-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXXI-1-5 CH ₃ H H CH ₂ Ph CH ₃ H F F OH XXXI-1-6 CH ₃ H H CH ₂ -indol-3-yl CH ₃ H F F OH XXXI-1-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH XXXI-1-8 CH ₃ * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-2-1 Et H H H CH ₃ H F F OH XXXI-2-2 Et H H CH ₃ CH ₃ H F F OH XXXI-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ H F F OH Xxxi-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH Xxxi-2-5 Et H H CH ₂ Ph CH ₃ H F F OH XXXI-2-6 Et H H CH ₂ -indol-3-yl CH ₃ H F F OH Xxxi-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH Xxxi-2-8 Et * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-3-1 ⁱ Pr H H H CH ₃ H F F OH XXXI-3-2 ⁱ Pr H H CH ₃ CH ₃ H F F OH XXXI-3-3 ⁱ Pr H H CH (CH ₃ ) ₂ CH ₃ H F F OH Xxxi-3-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H F F OH XXXI-3-5 ⁱ Pr H H CH ₂ Ph CH ₃ H F F OH XXXI-3-b ⁱ Pr H H CH ₂ -indol-3-yl CH ₃ H F F OH Xxxi-3-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ CH ₃ H F F OH Xxxi-3-8 ⁱ Pr * H * CH ₃ H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-4-1 ^t Bu H H H CH ₃ N F F IT XXXI-4-2 ^t Bu H H CH ₃ CH ₃ n F F IT XXXI-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ n F F IT XXXI-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT Xxxi-4-5 ^t Bu H H CH ₂ Ph CH ₃ n F F IT XXXI-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ n F F IT Xxxi-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXXI-4-8 ^t Bu * H * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-5-1 Ph H H H CH ₃ n F F IT XXXI-5-2 Ph H H CH ₃ CH ₃ n F F IT XXXI-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT XXXI-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT XXXI-5-5 Ph H H CH ₂ Ph CH ₃ n F F IT XXXI-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ n F F IT XXXI-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXXI-5-8 Ph * H * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-6-1 p-me-ph H H H CH ₃ N F F IT XXXI-6-2 p-me-ph H H CH ₃ CH ₃ N F F IT XXXI-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT XXXI-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT Xxxi-6-5 p-me-ph H H CH ₂ Ph CH ₃ N F F IT XXXI-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ N F F IT Xxxi-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT XXXI-6-8 p-me-ph * H * CH ₃ N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-7-1 p-f-ph H H H CH ₃ n F F IT XXXI-7-2 p-f-ph H H CH ₃ CH ₃ n F F IT XXXI-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ n F F IT XXXI-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ n F F IT XXXI-7-6 p-f-ph H H CH ₂ Ph CH ₃ n F F IT XXXI-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ n F F IT XXXI-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXXI-7-20 p-f-ph * H * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-8-1 p-Cl-Ph H H H CH ₃ N F F IT XXXI-8-2 p-Cl-Ph H H CH ₃ CH ₃ N F F IT XXXI-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT XXXI-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT Xxxi-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ N F F IT XXXI-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ N F F IT XXXI-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ n F F IT XXXI-8-8 p-Cl-Ph * H * CH ₃ n F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-9-1 p-Br-Ph H H H CH ₃ N F F IT XXXI-9-2 p-Br-Ph H H CH ₃ CH ₃ N F F IT XXXI-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ N F F IT XXXI-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F IT XXXI-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ N F F IT XXXI-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ N F F IT XXXI-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F IT XXXI-9-20 p-Br-Ph * H * CH ₃ N F F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-10-1 p-i-ph H H H CH ₃ N F F IT XXXI-10-2 p-i-ph H H CH ₃ CH ₃ N F F IT XXXI-10-3 p-i-ph H H CH (CH ₃ ) ₂ CH ₃ N F F it XXXI-10-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N F F it XXXI-10-5 p-i-ph H H CH ₂ Ph CH ₃ N F F it XXXI-10-6 p-i-ph H H CH ₂ -indol-3-yl CH ₃ N F F it XXXI-10-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ N F F it XXXI-10-8 p-i-ph * H * CH ₃ N F F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-11-1 CH ₃ N N n Et H F F OH XXXI-11-2 CH ₃ N N CH ₃ Et H F F OH XXXI-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H F F OH XXXI-11-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-11-5 CH ₃ N N CH ₂ Ph Et H F F OH XXXI-11-6 CH ₃ N N CH ₂ -indol-3-yl Et H F F OH XXXI-11-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-11-8 CH ₃ * N * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-12-1 Et H H H Et H F F OH XXXI-12-2 Et H H CH ₃ Et H F F OH XXXI-12-3 Et H H CH (CH ₃ ) ₂ Et H F F OH XXXI-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-12-5 Et H H CH ₂ Ph Et H F F OH XXXI-12-6 Et H H CH ₂ -indol-3-yl Et H F F OH XXXI-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-12-8 Et * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-13-1 ⁱ Pr H H H Et H F F OH XXXI-13-2 ⁱ Pr H H CH ₃ Et H F F OH XXXI-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et H F F OH XXXI-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-13-5 ⁱ Pr H H CH ₂ Ph Et H F F OH XXXI-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et H F F OH XXXI-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-13-8 fpr * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-14-1 ^t Bu H H H Et H F F OH XXXI-14-2 ^t Bu H H CH ₃ Et H F F OH XXXI-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H F F OH XXXI-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-14-5 ^t Bu H H CH ₂ Ph Et H F F OH XXXI-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H F F OH XXXI-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-14-8 ^t Bu * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-15-1 Ph H H H Et H F F OH XXXI-15-2 Ph H H CH ₃ Et H F F OH XXXX5-3 Ph H H CH (CH ₃ ) ₂ Et H F F OH XXXI-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-15-5 Ph H H CH ₂ Ph Et H F F OH XXXX5-6 Ph H H CH ₂ -indol-3-yl Et H F F OH XXXI-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-15-8 Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-16-1 p-me-ph H H H Et H F F OH XXXI-16-2 p-me-ph H H CH ₃ Et H F F OH XXXI-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H F F OH XXXX4-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH Xxxi-16-5 p-me-ph H H CH ₂ Ph Et H F F OH XXXI-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H F F OH XXXI-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-16-8 p-me-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-17-1 p-f-ph H H H Et H F F OH XXXI-17-2 p-f-ph H H CH ₃ Et H F F OH XXXI-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H F F OH XXXI-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-17-5 p-f-ph H H Chzph Et H F F OH XXXI-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H F F OH XXXI-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-17-8 p-f-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-18-1 p-Cl-Ph H H H Et H F F OH XXXI-18-2 p-Cl-Ph H H CH ₃ Et H F F OH XXXI-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H F F OH XXXI-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH Xxxi-18-5 p-Cl-Ph H H CH ₂ Ph Et H F F OH XXXI-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H F F OH XXXI-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-18-8 p-Cl-Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-19-1 p-Br-Ph H H H Et H F F OH XXXI-19-2 p-Br-Ph H H CH ₃ Et H F F OH XXXI-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H F F OH XXXI-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-19-5 p-Br-Ph H H CH ₂ Ph Et H F F OH XXXI-19-6 p-Br-Ph H H CH ₂ -indol-3-yl Et H F F OH XXXI-19-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-19-8 p-Br-Ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-20-1 p-i-ph H H H Et H F F OH XXXI-20-2 p-i-ph H H CH ₃ Et H F F OH XXXI-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H F F OH XXXI-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H F F OH XXXI-20-5 p-i-ph H H CH ₂ Ph Et H F F OH XXXI-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H F F OH XXXI-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H F F OH XXXI-20-8 p-i-ph * H * Et H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-21-1 CH ₃ N N n ⁱ Pr N F F IT XXXI-21-2 CH ₃ N N CH ₃ ⁱ Pr N F F IT XXXI-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr N F F it XXXI-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N F F it XXXI-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N F F it XXXI-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N F F it XXXI-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N F F it XXXI-21-8 CH ₃ * n * ⁱ Pr N F F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-22-1 Et H H H ⁱ Pr H F F OH XXXI-22-2 Et H H CH ₃ ⁱ Pr H F F OH XXXI-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-22-5 Et H H CH ₂ Ph ⁱ Pr H F F OH XXXI-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-22-8 Et * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-23-1 ⁱ Pr H H H ⁱ Pr H F F OH XXXI-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H F F OH XXXI-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H F F OH XXXI-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-23-8 ⁱ Pr * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-24-1 ^t Bu H H H ⁱ Pr H F F OH XXXI-24-2 ^t Bu H H CH ₃ ⁱ Pr H F F OH XXXI-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H F F OH XXXI-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-24-8 ^t Bu * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-25-1 Ph H H H ⁱ Pr H F F OH XXXI-25-2 Ph H H CH ₃ ⁱ Pr H F F OH XXXI-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-25-5 Ph H H CH ₂ Ph ⁱ Pr H F F OH XXXI-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-25-8 Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-26-1 p-me-ph H H H ⁱ Pr H F F OH XXXI-26-2 p-me-ph H H CH ₃ ⁱ Pr H F F OH XXXI-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H F F OH XXXI-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-26-8 p-me-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-27-1 p-f-ph H H H ⁱ Pr H F F OH XXXI-27-2 p-f-ph H H CH ₃ ⁱ Pr H F F OH XXXI-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H F F OH XXXI-27-6 p-f-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-27-8 p-f-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-28-1 p-Cl-Ph H H H ⁱ Pr H F F OH XXXI-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H F F OH XXXI-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H F F OH XXXI-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-28-8 p-Cl-Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-29-1 p-Br-Ph H H H ⁱ Pr H F F OH XXXI-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H F F OH XXXI-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H F F OH XXXI-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-29-8 p-Br-Ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-30-1 p-i-ph H H H ⁱ Pr H F F OH XXXI-30-2 p-i-ph H H CH ₃ ⁱ Pr H F F OH XXXI-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H F F OH XXXI-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H F F OH XXXI-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H F F OH XXXI-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H F F OH XXXI-30-8 p-i-ph * H * ⁱ Pr H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-31-1 CH ₃ N n n ⁿ Bu H F F OH XXXI-31-2 CH ₃ N n CH ₃ ⁿ Bu H F F OH XXXI-31-3 CH ₃ N n CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H F F OH XXXI-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-31-7 CH ₃ n n CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-31-8 CH ₃ * n * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-32-1 Et H H H ⁿ Bu H F F OH XXXI-32-2 Et H H CH ₃ ⁿ Bu H F F OH XXXI-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-32-5 Et H H CH ₂ Ph ⁿ Bu H F F OH XXXI-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-32-8 Et * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-33-1 ⁱ Pr H H H ⁿ Bu H F F OH XXXI-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H F F OH XXXI-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H F F OH XXXI-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-33-8 ⁱ Pr * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-34-1 ^t Bu H H H ⁿ Bu H F F OH XXXI-34-2 ^t Bu H H CH ₃ ⁿ Bu H F F OH XXXI-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H F F OH XXXI-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-34-8 ^t Bu * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-35-1 Ph H H H ⁿ Bu H F F OH XXXI-35-2 Ph H H CH ₃ ⁿ Bu H F F OH XXXI-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-35-5 Ph H H CH ₂ Ph ⁿ Bu H F F OH XXXI-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-35-8 Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-36-1 p-me-ph H H H ⁿ Bu H F F OH XXXI-36-2 p-me-ph H H CH ₃ ⁿ Bu H F F OH XXXI-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H F F OH XXXI-36-6 p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-36-8 p-me-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-37-1 p-f-ph H H H ⁿ Bu H F F OH XXXI-37-2 p-f-ph H H CH ₃ ⁿ Bu H F F OH XXXI-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H F F OH XXXI-37-b p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-37-8 p-f-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-38-1 p-Cl-Ph H H H ⁿ Bu H F F OH XXXI-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H F F OH XXXI-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H F F OH XXXI-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-38-8 p-Cl-Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-39-1 p-Br-Ph H H H ⁿ Bu H F F OH XXXI-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H F F OH XXXI-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H F F OH XXXI-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-39-8 p-Br-Ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-40-1 p-i-ph H H H ⁿ Bu H F F OH XXXI-40-2 p-i-ph H H CH ₃ ⁿ Bu H F F OH XXXI-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H F F OH XXXI-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H F F OH XXXI-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H F F OH XXXI-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H F F OH XXXI-40-8 p-i-ph * H * ⁿ Bu H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-41-1 CH ₃ N N n Bz H F F OH XXXI-41-2 CH ₃ N N CH ₃ Bz H F F OH XXXI-41-3 CH ₃ N N CH (CH ₃ ) ₂ Bz H F F OH XXXI-41-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-41-5 CH ₃ N n CH ₂ Ph Bz H F F OH XXXI-41-6 CH ₃ N n CH ₂ -indol-3-yl Bz H F F OH XXXI-41-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-41-8 CH ₃ * n * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-42-1 Et H H H Bz H F F OH XXXI-42-2 Et H H CH ₃ Bz H F F OH XXXI-42-3 Et H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-42-5 Et H H CH ₂ Ph Bz H F F OH XXXI-42-6 Et H H CH ₂ -indol-3-yl Bz H F F OH XXXI-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-42-8 Et * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-43-1 ⁱ Pr H H H Bz H F F OH XXXI-43-2 ⁱ Pr H H CH ₃ Bz H F F OH XXXI-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-43-5 ⁱ Pr H H CH ₂ Ph Bz H F F OH XXXI-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H F F OH XXXI-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-43-8 ⁱ Pr * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-44-1 ^t Bu H H H Bz H F F OH XXXI-44-2 ^t Bu H H CH ₃ Bz H F F OH XXXI-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-44-5 ^t Bu H H CH ₂ Ph Bz H F F OH XXXI-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H F F OH XXXI-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-44-8 ^t Bu * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-45-1 Ph H H H Bz H F F OH XXXI-45-2 Ph H H CH ₃ Bz H F F OH XXXI-45-3 Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-4S-5 Ph H H CH ₂ Ph Bz H F F OH XXXI-45-6 Ph H H CH ₂ -indol-3-yl Bz H F F OH XXXI-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-45-8 Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-46-1 p-me-ph H H H Bz H F F OH XXXI-46-2 p-me-ph H H CH ₃ Bz H F F OH XXXI-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-46-5 p-me-ph H H CH ₂ Ph Bz H F F OH XXXI-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H F F OH XXXI-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-46-8 p-me-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-47-1 p-f-ph H H H Bz H F F OH XXXI-47-2 p-f-ph H H CH ₃ Bz H F F OH XXXI-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-47-5 p-f-ph H H CH ₂ Ph Bz H F F OH XXXI-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H F F OH XXXI-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-47-8 p-f-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-48-1 p-Cl-Ph H H H Bz H F F OH XXXI-48-2 p-Cl-Ph H H CH ₃ Bz H F F OH XXXI-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-48-5 p-Cl-Ph H H CH ₂ Ph Bz H F F OH XXXI-48-b p-Cl-Ph H H CH ₂ -indol-3-yl Bz H F F OH XXXI-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-48-8 p-Cl-Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXI-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-49-1 p-Br-Ph H H H Bz H F F OH XXXI-49-2 p-Br-Ph H H CH ₃ Bz H F F OH XXXI-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-49-5 p-Br-Ph H H CH ₂ Ph Bz H F F OH XXXI-49-6 p-Br-Ph H H CH ₂ -vdol-3-yl Bz H F F OH XXXI-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-49-8 p-Br-Ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXI-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXI-50-1 p-i-ph H H H Bz H F F OH XXXI-50-2 p-i-ph H H CH ₃ Bz H F F OH XXXI-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H F F OH XXXI-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H F F OH XXXI-50-5 p-i-ph H H CH ₂ Ph Bz H F F OH XXXI-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H F F OH XXXI-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H F F OH XXXI-50-8 p-i-ph * H * Bz H F F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-1. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-1-1 CH ₃ N N n CH ₃ N N F IT XXXII-1-2 CH ₃ N N CH ₃ CH ₃ N N F IT XXXII-1-3 CH ₃ N N CH (CH ₃ ) ₂ CH ₃ N N F IT XXXII-1-4 CH ₃ N N CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT Xxxii-1-5 CH ₃ N N CH ₂ Ph CH ₃ N N F IT XXXII-1-6 CH ₃ N N CH ₂ -indol-3-yl CH ₃ N N F IT XXXII-1-7 CH ₃ N N CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT XXXII-1-8 CH ₃ * N * CH ₃ N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-2. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y Xxxii-2-1 Et H H H CH ₃ N N F it Xxxii-2-2 Et H H CH ₃ CH ₃ N N F it XXXII-2-3 Et H H CH (CH ₃ ) ₂ CH ₃ N n F IT XXXII-2-4 Et H H CH ₂ CH (CH ₃ ) ₂ CH ₃ N n F IT XXXII-2-5 Et H H CH ₂ Ph CH ₃ N n F IT XXXII-2-6 Et H H CH ₂ -indol-3-yl CH ₃ N n F IT XXXII-2-7 Et H H CH ₂ CH ₂ SCH ₃ CH ₃ N n F IT Xxxii-2-8 Et * H * CH ₃ N n F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-3. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-3-1 ⁱ Pr N n n CH ₃ N N F IT XXXII-3-2 ⁱ Pr N n CH ₃ CH ₃ N N F IT XXXII-3-Z ⁱ Pr N n CH (CH ₃ ) ₂ CH ₃ N N F IT XXXII-3-4 ⁱ Pr N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXXII-3-5 ⁱ Pr N n CH ₂ Ph CH ₃ N N F IT XXXII-3-6 ⁱ Pr N n CH ₂ -indol-3-yl CH ₃ N N F IT XXXII-3-7 ⁱ Pr n n CH ₂ CH ₂ SCH ₃ CH ₃ N N F it XXXII-3-8 ⁱ Pr n * CH ₃ N N F it * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-4. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-4-1 ^t Bu H H H CH ₃ H H F OH Xxxii-4-2 ^t Bu H H CH ₃ CH ₃ H H F OH Xxxii-4-3 ^t Bu H H CH (CH ₃ ) ₂ CH ₃ H H F OH Xxxii-4-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-4-5 ^t Bu H H CH ₂ Ph CH ₃ H H F OH XXXII-4-6 ^t Bu H H CH ₂ -indol-3-yl CH ₃ H H F OH XXXII-4-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH XXXII-4-8 ^t Bu * H * CH ₃ H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-5. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-5-1 Ph H H H CH ₃ H H F OH XXXII-5-2 Ph H H CH ₃ CH ₃ H H F OH XXXII-5-3 Ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-5-4 Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-5-5 Ph H H CH ₂ Ph CH ₃ H H F OH XXXII-5-6 Ph H H CH ₂ -indol-3-yl CH ₃ H H F OH XXXII-5-7 Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH XXXII-5-8 Ph * H * CH ₃ H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-6. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-6-1 p-me-ph H H H CH ₃ H H F OH XXXII-6-2 p-me-ph H H CH ₃ CH ₃ H H F OH XXXII-6-3 p-me-ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-6-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-6-5 p-me-ph H H CH ₂ Ph CH ₃ H H F OH XXXII-6-6 p-me-ph H H CH ₂ -indol-3-yl CH ₃ H H F OH XXXII-6-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH XXXII-6-8 p-me-ph * H * CH ₃ H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-7. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-7-1 p-f-ph H H H CH ₃ H H F OH XXXII-7-2 p-f-ph H H CH ₃ CH ₃ H H F OH XXXII-7-3 p-f-ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH Xxxii-7-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-7-6 p-f-ph H H CH ₂ Ph CH ₃ H H F OH Xxxii-7-7 p-f-ph H H CH ₂ -indol-3-yl CH ₃ H H F OH XXXII-7-8 p-f-ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH Xxxii-7-20 p-f-ph * H * CH ₃ H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-8. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-8-1 p-Cl-Ph H H H CH ₃ H H F OH XXXII-8-2 p-Cl-Ph H H CH ₃ CH ₃ H H F OH XXXII-8-3 p-Cl-Ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-8-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH Xxxii-8-5 p-Cl-Ph H H CH ₂ Ph CH ₃ H H F OH XXXII-8-6 p-Cl-Ph H H CH ₂ -indol-3-yl CH ₃ H H F OH XXXII-8-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH Xxxii-8-8 p-Cl-Ph * H * CH ₃ H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-9. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-9-1 p-Br-Ph H H H CH ₃ H H F OH XXXII-9-2 p-Br-Ph H H CH ₃ CH ₃ H H F OH XXXII-9-3 p-Br-Ph H H CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-9-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ CH ₃ H H F OH XXXII-9-6 p-Br-Ph H H CH ₂ Ph CH ₃ H H F OH XXXII-9-7 p-Br-Ph H H CH ₂ -indol-3-yl CH ₃ H H F OH XXXII-9-8 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ CH ₃ H H F OH XXXII-9-20 p-Br-Ph * H * CH ₃ H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-10. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-10-1 p-1-ph N N N CH ₃ N N F IT XXXII-10-2 p-1-ph N N CH ₃ CH ₃ N N F IT XXXII-10-3 p-1-ph N N CH (CH ₃ ) ₂ CH ₃ N N F IT XXXII-10-4 p-1-ph N n CH ₂ CH (CH ₃ ) ₂ CH ₃ N N F IT XXXII-10-5 p-1-ph N n CH ₂ Ph CH ₃ N N F IT XXXII-10-6 p-1-ph N n CH ₂ -indol-3-yl CH ₃ N N F IT XXXII-10-7 p-1-ph N n CH ₂ CH ₂ SCH ₃ CH ₃ N N F IT XXXII-10-8 p-1-ph n * CH ₃ N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-11. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-11-1 CH ₃ N n n Et H H F OH XXXII-11-2 CH ₃ N n CH ₃ Et H H F OH XXXII-11-3 CH ₃ N n CH (CH ₃ ) ₂ Et H H F OH XXXII-11-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-11-5 CH ₃ N n CH ₂ Ph Et H H F OH XXXII-11-6 CH ₃ N n CH ₂ -indol-3-yl Et H H F OH XXXII-11-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-11-8 CH ₃ * n * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-12. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-12-1 Et H H H Et H H F OH XXXII-12-2 Et H H CH ₃ Et H H F OH XXXII-12-3 Et H H CH (CH ₃ ) ₂ Et H H F OH XXXII-12-4 Et H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH Xxxii-12-5 Et H H CH ₂ Ph Et H H F OH XXXII-12-6 Et H H CH ₂ -indol-3-yl Et H H F OH XXXII-12-7 Et H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-12-8 Et * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-13. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-13-1 ⁱ Pr H H H Et H H F OH XXXII-13-2 ⁱ Pr H H CH ₃ Et H H F OH XXXII-13-3 ⁱ Pr H H CH (CH ₃ ) ₂ Et H H F OH XXXII-13-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-13-5 ⁱ Pr H H CH ₂ Ph Et H H F OH XXXII-13-6 ⁱ Pr H H CH ₂ -indol-3-yl Et H H F OH XXXII-13-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-13-8 ⁱ Pr * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-14. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-14-1 ^t Bu H H H Et H H F OH XXXII-14-2 ^t Bu H H CH ₃ Et H H F OH XXXII-14-3 ^t Bu H H CH (CH ₃ ) ₂ Et H H F OH XXXII-14-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-14-5 ^t Bu H H CH ₂ Ph Et H H F OH XXXII-14-6 ^t Bu H H CH ₂ -indol-3-yl Et H H F OH XXXII-14-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-14-8 ^t Bu * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-15. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-15-1 Ph H H n Et H H F OH XXXII-15-2 Ph H H CH ₃ Et H H F OH XXXII-15-3 Ph H H CH (CH ₃ ) ₂ Et H H F OH XXXII-15-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-15-5 Ph H H CH ₂ Ph Et H H F OH XXXII-15-6 Ph H H CH ₂ -indol-3-yl Et H H F OH XXXII-15-7 Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-15-8 Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-16. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-16-1 p-me-ph H H H Et H H F OH XXXII-16-2 p-me-ph H H CH ₃ Et H H F OH XXXII-16-3 p-me-ph H H CH (CH ₃ ) ₂ Et H H F OH XXXII-16-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-16-5 p-me-ph H H CH ₂ Ph Et H H F OH XXXII-16-6 p-me-ph H H CH ₂ -indol-3-yl Et H H F OH XXXII-16-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-16-8 p-me-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-17. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-17-1 p-f-ph H H H Et H H F OH XXXII-17-2 p-f-ph H H CH ₃ Et H H F OH XXXII-17-3 p-f-ph H H CH (CH ₃ ) ₂ Et H H F OH XXXII-17-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-17-5 p-f-ph H H CH ₂ Ph Et H H F OH XXXII-17-6 p-f-ph H H CH ₂ -indol-3-yl Et H H F OH XXXII-17-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-17-8 p-f-ph * H * Et H H F OH Table XXXII-18. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-18-1 p-Cl-Ph H H H Et H H F OH XXXII-18-2 p-Cl-Ph H H CH ₃ Et H H F OH XXXII-18-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Et H H F OH XXXII-18-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-18-5 p-Cl-Ph H H CH ₂ Ph Et H H F OH XXXII-18-6 p-Cl-Ph H H CH ₂ -indol-3-yl Et H H F OH XXXII-18-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-18-8 p-Cl-Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-19. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-19-1 p-Br-Ph H H H Et H H F OH XXXII-19-2 p-Br-Ph H H CH ₃ Et H H F OH XXXH-19-3 p-Br-Ph H H CH (CH ₃ ) ₂ Et H H F OH XXXII-19-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-19-5 p-Br-Ph H H CH ₂ Ph Et H H F OH XXXII-19-b p-Br-Ph H H CH ₂ -indol-3-yl Et H H F OH XXXIM9-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-19-8 p-Br-Ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-20. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-20-1 p-i-ph H H H Et H H F OH XXXII-20-2 p-i-ph H H CH ₃ Et H H F OH XXXII-20-3 p-i-ph H H CH (CH ₃ ) ₂ Et H H F OH XXXII-20-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Et H H F OH XXXII-20-5 p-i-ph H H CH ₂ Ph Et H H F OH XXXII-20-6 p-i-ph H H CH ₂ -indol-3-yl Et H H F OH XXXII-20-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Et H H F OH XXXII-20-8 p-i-ph * H * Et H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-21. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-21-1 CH ₃ N N n ⁱ Pr N N F IT XXXII-21-2 CH ₃ N N CH ₃ ⁱ Pr N N F IT XXXII-21-3 CH ₃ N n CH (CH ₃ ) ₂ ⁱ Pr N N F IT XXXII-21-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁱ Pr N N F IT XXXII-21-5 CH ₃ N n CH ₂ Ph ⁱ Pr N N F IT XXXII-21-6 CH ₃ N n CH ₂ -indol-3-yl ⁱ Pr N N F IT XXXII-21-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁱ Pr N N F IT XXXII-21-8 CH ₃ * n * ⁱ Pr N N F IT * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-22. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-22-1 Et H H H ⁱ Pr H H F OH XXXII-22-2 Et H H CH ₃ ⁱ Pr H H F OH XXXII-22-3 Et H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-22-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-22-5 Et H H CH ₂ Ph ⁱ Pr H H F OH XXXII-22-6 Et H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-22-7 Et H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-22-8 Et * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-23. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-23-1 ⁱ Pr H H H ⁱ Pr H H F OH XXXII-23-2 ⁱ Pr H H CH ₃ ⁱ Pr H H F OH XXXII-23-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-23-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-23-5 ⁱ Pr H H CH ₂ Ph ⁱ Pr H H F OH XXXII-23-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-23-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-23-8 ⁱ Pr * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-24. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-24-1 ^t Bu H H H ⁱ Pr H H F OH XXXII-24-2 ^t Bu H H CH ₃ ⁱ Pr H H F OH XXXII-24-3 ^t Bu H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-24-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-24-5 ^t Bu H H CH ₂ Ph ⁱ Pr H H F OH XXXII-24-6 ^t Bu H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-24-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-24-8 ^t Bu * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-25. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-25-1 Ph H H H ⁱ Pr H H F OH XXXII-25-2 Ph H H CH ₃ ⁱ Pr H H F OH XXXII-25-3 Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-25-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-25-5 Ph H H CH ₂ Ph ⁱ Pr H H F OH XXXII-25-6 Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-25-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-25-8 Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-26. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-26-1 p-me-ph H H H ⁱ Pr H H F OH XXXII-26-2 p-me-ph H H CH ₃ ⁱ Pr H H F OH XXXII-26-3 p-me-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-26-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-26-5 p-me-ph H H CH ₂ Ph ⁱ Pr H H F OH XXXII-26-6 p-me-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-26-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-26-8 p-me-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-27. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-27-1 p-f-ph H H H ⁱ Pr H H F OH XXXII-27-2 p-f-ph H H CH ₃ ⁱ Pr H H F OH XXXII-27-3 p-f-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-27-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-27-5 p-f-ph H H CH ₂ Ph ⁱ Pr H H F OH XXXII-27-6 p-f-ph H H CH ₂ -indol-3-yl * pr H H F OH XXXII-27-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-27-8 p-f-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-28. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-28-1 p-Cl-Ph H H H ⁱ Pr H H F OH XXXII-28-2 p-Cl-Ph H H CH ₃ ⁱ Pr H H F OH XXXII-28-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-28-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-28-5 p-Cl-Ph H H CH ₂ Ph ⁱ Pr H H F OH XXXII-28-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-28-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-28-8 p-Cl-Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-29. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-29-1 p-Br-Ph H H H ⁱ Pr H H F OH XXXII-29-2 p-Br-Ph H H CH ₃ ⁱ Pr H H F OH XXXII-29-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-29-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-29-5 p-Br-Ph H H CH ₂ Ph ⁱ Pr H H F OH XXXII-29-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-29-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-29-8 p-Br-Ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-30. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-30-1 p-i-ph H H H ⁱ Pr H H F OH XXXII-30-2 p-i-ph H H CH ₃ ⁱ Pr H H F OH XXXII-30-3 p-i-ph H H CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-30-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁱ Pr H H F OH XXXII-30-5 p-i-ph H H CH ₂ Ph ⁱ Pr H H F OH XXXII-30-6 p-i-ph H H CH ₂ -indol-3-yl ⁱ Pr H H F OH XXXII-30-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁱ Pr H H F OH XXXII-30-8 p-i-ph * H * ⁱ Pr H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-31. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-31-1 CH ₃ N N n ⁿ Bu H H F OH XXXII-31-2 CH ₃ N N CH ₃ ⁿ Bu H H F OH XXXII-31-3 CH ₃ N N CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-31-4 CH ₃ N n CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-31-5 CH ₃ N n CH ₂ Ph ⁿ Bu H H F OH XXXII-31-6 CH ₃ N n CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-31-7 CH ₃ N n CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-31-8 CH ₃ * n * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-32. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-32-1 Et H H H ⁿ Bu H H F OH XXXII-32-2 Et H H CH ₃ ⁿ Bu H H F OH XXXII-32-3 Et H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-32-4 Et H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-32-5 Et H H CH ₂ Ph ⁿ Bu H H F OH XXXII-32-6 Et H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-32-7 Et H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-32-8 Et * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-33. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-33-1 ⁱ Pr H H H ⁿ Bu H H F OH XXXII-33-2 ⁱ Pr H H CH ₃ ⁿ Bu H H F OH XXXII-33-3 ⁱ Pr H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-33-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-33-5 ⁱ Pr H H CH ₂ Ph ⁿ Bu H H F OH XXXII-33-6 ⁱ Pr H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-33-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-33-8 ⁱ Pr * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-34. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-34-1 ^t Bu H H H ⁿ Bu H H F OH XXXII-34-2 ^t Bu H H CH ₃ ⁿ Bu H H F OH XXXII-34-3 ^t Bu H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-34-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-34-5 ^t Bu H H CH ₂ Ph ⁿ Bu H H F OH XXXII-34-6 ^t Bu H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-34-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-34-8 ^t Bu * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-35. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-35-1 Ph H H H ⁿ Bu H H F OH XXXII-35-2 Ph H H CH ₃ ⁿ Bu H H F OH XXXII-35-3 Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-35-4 Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-35-5 Ph H H CH ₂ Ph ⁿ Bu H H F OH XXXII-35-6 Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-35-7 Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-35-8 Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-36. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-36-1 p-me-ph H H H ⁿ Bu H H F OH XXXII-36-2 p-me-ph H H CH ₃ ⁿ Bu H H F OH XXXII-36-3 p-me-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-36-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-36-5 p-me-ph H H CH ₂ Ph ⁿ Bu H H F OH XXXII-36-b p-me-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-36-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-36-8 p-me-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-37. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-37-1 p-f-ph H H H ⁿ Bu H H F OH XXXII-37-2 p-f-ph H H CH ₃ ⁿ Bu H H F OH XXXII-37-3 p-f-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-37-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-37-5 p-f-ph H H CH ₂ Ph ⁿ Bu H H F OH XXXII-37-6 p-f-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-37-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-37-8 p-f-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-38. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-38-1 p-Cl-Ph H H H ⁿ Bu H H F OH XXXII-38-2 p-Cl-Ph H H CH ₃ ⁿ Bu H H F OH XXXII-38-3 p-Cl-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-38-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-38-5 p-Cl-Ph H H CH ₂ Ph ⁿ Bu H H F OH XXXII-38-6 p-Cl-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-38-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-38-8 p-Cl-Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-39. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-39-1 p-Br-Ph H H H ⁿ Bu H H F OH XXXII-39-2 p-Br-Ph H H CH ₃ ⁿ Bu H H F OH XXXII-39-3 p-Br-Ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-39-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-39-5 p-Br-Ph H H CH ₂ Ph ⁿ Bu H H F OH XXXII-39-6 p-Br-Ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-39-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-39-8 p-Br-Ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-40. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-40-1 p-i-ph H H H ⁿ Bu H H F OH XXXII-40-2 p-i-ph H H CH ₃ ⁿ Bu H H F OH XXXII-40-3 p-i-ph H H CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-40-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ ⁿ Bu H H F OH XXXII-40-5 p-i-ph H H CH ₂ Ph ⁿ Bu H H F OH XXXII-40-6 p-i-ph H H CH ₂ -indol-3-yl ⁿ Bu H H F OH XXXII-40-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ ⁿ Bu H H F OH XXXII-40-8 p-i-ph * H * ⁿ Bu H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-41. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-41-1 CH ₃ H H H Bz H H F OH XXXII-41-2 CH ₃ H H CH ₃ Bz H H F OH XXXII-41-3 CH ₃ H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-41-4 CH ₃ H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-41-5 CH ₃ H H CH ₂ Ph Bz H H F OH XXXII-41-6 CH ₃ H H CH ₂ -indol-3-yl Bz H H F OH XXXII-41-7 CH ₃ H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-41-8 CH ₃ H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-42. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-42-1 Et H H H Bz H H F OH XXXII-42-2 Et H H CH ₃ Bz H H F OH XXXII-42-3 Et H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-42-4 Et H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-42-5 Et H H CH ₂ Ph Bz H H F OH XXXII-42-6 Et H H CH ₂ -indol-3-yl Bz H H F OH XXXII-42-7 Et H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-42-8 Et * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-43. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-43-1 ⁱ Pr H H H Bz H H F OH XXXII-43-2 ⁱ Pr H H CH ₃ Bz H H F OH XXXII-43-3 ⁱ Pr H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-43-4 ⁱ Pr H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-43-5 ⁱ Pr H H CH ₂ Ph Bz H H F OH XXXII-43-6 ⁱ Pr H H CH ₂ -indol-3-yl Bz H H F OH XXXII-43-7 ⁱ Pr H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-43-8 ⁱ Pr * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-44. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-44-1 ^t Bu H H H Bz H H F OH XXXII-44-2 ^t Bu H H CH ₃ Bz H H F OH XXXII-44-3 ^t Bu H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-44-4 ^t Bu H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-44-5 ^t Bu H H CH ₂ Ph Bz H H F OH XXXII-44-6 ^t Bu H H CH ₂ -indol-3-yl Bz H H F OH XXXII-44-7 ^t Bu H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-44-8 ^t Bu * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-45. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-45-1 Ph H H H Bz H H F OH XXXII-45-2 Ph H H CH ₃ Bz H H F OH XXXII-45-3 Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-45-4 Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-45-5 Ph H H CH ₂ Ph Bz H H F OH XXXII-45-6 Ph H H CH ₂ -indol-3-yl Bz H H F OH XXXII-45-7 Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-45-8 Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-46. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-46-1 p-me-ph H H H Bz H H F OH XXXII-46-2 p-me-ph H H CH ₃ Bz H H F OH XXXII-46-3 p-me-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-46-4 p-me-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-46-5 p-me-ph H H CH ₂ Ph Bz H H F OH XXXII-46-6 p-me-ph H H CH ₂ -indol-3-yl Bz H H F OH XXXII-46-7 p-me-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-46-8 p-me-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-47. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-47-1 p-f-ph H H H Bz H H F OH XXXII-47-2 p-f-ph H H CH ₃ Bz H H F OH XXXII-47-3 p-f-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-47-4 p-f-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-47-5 p-f-ph H H CH ₂ Ph Bz H H F OH XXXII-47-6 p-f-ph H H CH ₂ -indol-3-yl Bz H H F OH XXXII-47-7 p-f-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-47-8 p-f-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-48. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-48-1 p-Cl-Ph H H H Bz H H F OH XXXII-48-2 p-Cl-Ph H H CH ₃ Bz H H F OH XXXII-48-3 p-Cl-Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-48-4 p-Cl-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-48-5 p-Cl-Ph H H CH ₂ Ph Bz H H F OH XXXII-48-6 p-Cl-Ph H H CH ₂ -indol-3-yl Bz H H F OH XXXII-48-7 p-Cl-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-48-8 p-Cl-Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring.

Table XXXII-49. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-49-1 p-Br-Ph H H H Bz H H F OH XXXII-49-2 p-Br-Ph H H CH ₃ Bz H H F OH XXXII-49-3 p-Br-Ph H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-49-4 p-Br-Ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-49-5 p-Br-Ph H H CH ₂ Ph Bz H H F OH XXXII-49-6 p-Br-Ph H H CH ₂ -indol-3-yl Bz H H F OH XXXII-49-7 p-Br-Ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-49-8 p-Br-Ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Table XXXII-50. No. R ¹ R ² R ^3a R ^3b R ⁴ R ⁵ R ⁶ X Y XXXII-50-1 p-i-ph H H H Bz H H F OH XXXII-50-2 p-i-ph H H CH ₃ Bz H H F OH XXXII-50-3 p-i-ph H H CH (CH ₃ ) ₂ Bz H H F OH XXXII-50-4 p-i-ph H H CH ₂ CH (CH ₃ ) ₂ Bz H H F OH XXXII-50-5 p-i-ph H H CH ₂ Ph Bz H H F OH XXXII-50-6 p-i-ph H H CH ₂ -indol-3-yl Bz H H F OH XXXII-50-7 p-i-ph H H CH ₂ CH ₂ SCH ₃ Bz H H F OH XXXII-50-8 p-i-ph * H * Bz H H F OH * R ² and R ^{3b are} connected to each other via (CH ₂ ) ₃ to form a five-membered ring. Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 13 Ph H H Me Et 1 H-NMR (DMSO-d ₆ ) δ 1.12-1.16 (m, 3H), 1.20-1.28 (m, 6H), 3.70-3.90 (m, 2H), 4.00-4.08 (m, 3H), 4.18-4.45 ( m, 2H), 5.52-5.58 (m, 1H), 5.85-5.98 (m, 1H), 6.00-6.20 (m, 2H), 7.16-7.23 (m, 3H), 7.37-7.40 (m, 2H), 7.54-7.60 (m, 1H); 11.54 (s. 1H); MC, m / e 516.1 (M + 1) + fourteen 1-napth H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.18-1.30 (m, 6H), 3.784.10 (m, 3H), 4.38-4.49 (m, 2H), 4.99-5.11 (m, 2H), 5.28-5.40 ( m, 1H), 5.85-6.10 (m. 2H), 6.30-6.41 (m, 1H), 7.28-7.32 (m, 5H), 7.41-7.60 (m, 5H), 7.73-7.76 (m, 1H), 7.94-8.11 (m, 1H), 8.13-8.15 (m, 1H), 11.50 (s. 1H); MC, m / e 628.4 (M + 1) + fifteen Ph H H H Me 1 H-NMR (DMSO-d ₆ ) δ 1.22 (d, J = 22.4 Hz. 3H), 3.59 (s, 3H), 3.63-3.69 (m, 2H), 3.74-3.8 (m, 1H), 4.02 (d , J = 11.2 Hz. 1H). 4.23-4.28 (m, 1H), 4.404.43 (m, 1H), 5.57-5.60 (m, 1H), 5.89 (d. J = 6.8 Hz, 1H), 6.00-6.06 (m, 2H), 7.15- 7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.52 (d, J = 8 Hz, 1H), 11.52 (s, 1H); MC, m / e 487.97 (M + 1) + 16 2,4-Cl- H H Me Me 1 H NMR (DMSO-d ₆ ) δ 1.22-1.28 (m, 6H), 3.57-3.60 (m, 3H), 3.84-3.92

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS Ph (m, 2H), 4.00-4.04 (m. 1H). 4.31-4.44 (m, 2H), 5.54-5.61 (m, 1H), 5.85-6.10 (m, 2H), 6.32-6.43 (m, 1H), 7.44-7.54 (m, 3H), 7.72-7.75 (m . 1H), 11.54 (s. 1H); MC, m / e 570.2 (M + 1) + 17 1-napth H H Me Me 1 H-NMR (DMSO-d ₆ ) δ 1.15-1.27 (m, 6H), 3.51-3.55 (d, 3H), 3.85-3.96 (m, 2H), 4.00-4.10 (m, 1H), 4.30-4.46 ( m, 2H), 5.31-5.39 (m, 1H), 5.89-6.05 (m, 2H), 6.22-6.34 (m, 1H), 7.44-7.60 (m, 5H). 7.73-7.77 (m, 1H), 7.93-7.96 (m, 1H), 8.12-8.14 (m, 1H) .11.50 (s.1H); MC. m / e 552.1 (M + 1) + eighteen Ph H * Me 1 H NMR (DMSO-d ₆ ) δ 1.19 (d. J = 22.8 Hz. 3H), 1.69-1.84 (m, 3H). 1.99-2.04 (m, 1H), 3.16-3.21 (m, 2H), 3.58 (s, 3H), 3.68-3.8 (m, 1H), 4.00 (m, 1H), 4.01-4.13 (m, 1H), 4.22-4.25 (m, 1 H), 4.5 (d, J = 11.2 Hz, 1H), 5.54 (d, J = 8.0 Hz, 1H), 5.86 (s, 1H), 5.6 (d, J = 19.6 Hz, 1H), 7.15-7.2 (m, 3H), 7.34 (t, J = 8.0 Hz, 2H), 7.51 (d. J = 8.0 Hz, 1H), 11.38 (s, 1H); MC, m / e 527.93 (M + 1) + 19 Ph H H Me n-bu 1 H-NMR (DMSO-d ₆ ) δ 0.80-0.90 (m, 3H), 1.20-1.35 (m, 8H), 1.48-155 (m, 2H), 3.78-3.88 (m, 2H), 3.95-4.08 ( m, 3H), 4.22-4.45 (m, 2H), 555-557 (t, 1H), 5.85-6.18 (m, 3H), 7.14-7.23 (m, 3H), 7.35-7.40 (m, 2H), 7.51-7.60 (d, 1H), 1150 (s.lH); MC, m / e 544.2 (M + 1) + twenty Ph H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.20-1.30 (m, 6H), 3.72-4.05 (m, 3H), 4.23-4.27 (m, 1H), 4.32-4.45 (m, 1H), 5.07-5.10 ( t, 2H), 5.52-5.56 (1, 1H), 5.86-6.10 (m, 2H), 6.13-6.21 (m, 1H), 7.15-7.21 (m, 3H), 7.29-7.40 (m, 7H), 7.51-7.56 (d, 1H), 11.50 (s. 1H); MC, m / e 578.2 (M + 1) + 21 4-f-ph H H Me Me 1 H-NMR (DMSO-d ₆ ) δ 1.28-1.34 (m, 6H), 3.65 (d, J = 4 Hz, 3H), 3.85-3.96 (m, 2H), 4.06-4.12 (m, 1H), 4.30 -4.34 (m, 1H), 4.40-4.47 (m, 1H), 5.62-5.67 (m, 1H), 5.94-6.01 (m, 1H), 6.09 (d, J = 18.8 Hz, 1H), 6.17-6.26 (m, 1H), 7.27-7.33 (m, 4H), 7.62 (d, J = 7.6 Hz, 1H), 11.61 (s, 1H); MC, m / e 519.94 (M + 1) + 22 4-cl-ph H H Me Me 1 H-NMR (DMSO-d ₆ ) δ 1.22-1.28 (m, 6H), 358 (d, 2H), 3.70-3.95 (m, 2H), 3.95-4.08 (m, 1H), 4.23-4.45 (m, 2H), 5.55-5.61 (t, 1H), 5.85-6.10 (m, 2H), 6.15-6.23 (m, 1H), 7.20-7.26 (m, 2H), 7.43-7.46 (m, 2H), 7.54- 757 (d, 1H); 11.50 (s. 1H); MC, m / e 536.1 (M + 1) + 23 3,4-Cl-Ph H H Me Me 1 H-NMR (DMSO-d ₆ ) δ 1.13 (m, 6H), 3.49 (s, 3H), 3.61-3.85 (m, 2H), 3.90-3.93 (m, 1H), 4.16-4.22 (m, 1H) , 4.27-4.31 (m, 1H), 5.47-5.52 (m, 1H), 5.82 (d, J = 11.6 Hz, 1H), 5.93 (d, J = 19.2 Hz, 1H), 6.15-6.25 (m, 1H ), 7.13 (t, J = 9.6 Hz, 1H), 7.43 (d, J = 12 Hz, 2H), 757 (d, J = 6.0 Hz, 1H), 11.43 (s, 1H); MC, m / e 569.85 (M + 1) + 24 Ph H H Me 2-bu 1 H NMR (DMSO-d ₆ ) δ 0.83 (d, J = 6.8 Hz, 6H), 1.20-1.26 (m, 6H), 1.79-1.86 (m, 1H), 3.73-3.90 (m, 4H), 4.01 (t, J = 11.2 Hz, 1H), 4.21-4.28 (m, 1H), 4.33-4.42 (m, 1H), 5.54 (t, J = 7.6 Hz, 1H), 5.85-5.92 (m, 1H), 5.99-6.13 (m, 2H), 7.19 (t, J = 8 Hz, 3H), 7.36 (t, J = 7.6 Hz, 2H), 7.53 (d, J = 7.6 Hz, 1H), 11.52 (s, 1H ); MC, m / e 544.00 (M + 1) + 25 Ph H H Me i-pr 1H-NMR (DMSO-d ₆ ) δ 1.13-1.28 (m, 12H), 3.74-3.81 (m, 2H), 3.95-4.08 (m, 1H), 4.20-4.45 (m, 2H), 4.83-4.87 ( m, 1H), 5.52-558 (m, 1H), 5.84-6.15 (m, 3H), 7.17-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.54-7.57 (m, 1H), 1150 (s. 1H); MC, m / e 530.2 (M + 1) + 26 4-MeO- H H Me n-bu 1 H NMR (400 MHz, DMSO-d ₆ ): δ = 0.78-0.82 (m, 3H), 1.29-1.47 (m,

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS Ph 8H), 1.49-1.54 (m, 2H), 3.66-3.87 (m, 5H), 3.96-4.02 (m, 3H), 4.21-4.39 (m, 2H), 557 (t, J = 12.0 Hz, 1H) , 5.84-6.05 (m, 3H), 6.90 (dd, J1 = 8.0 Hz, J4 = 4.0 Hz, 2H), 7.09-7.14 (dd, J1 = 16.0 Hz, 12 = 4.0 Hz, 2H), 7.55 (d, J = 8.0 Hz, 1H), 11.48-11.62 (s, 1H) 27 4-f-ph H H Me Et 1H-NMR (DMSO-d ₆ ) δ 1.12-1.28 (m, 9H), 3.72-3.94 (m, 2H), 3.98-4.10 (m, 3H), 4.214.42 (m, 2H), 5.55-5.61 ( t, 1H), 5.85-6.20 (m, 3H), 7.18-7.25 (m, 4H), 7.55-7.58 (d, 1H), 11.50 (s. 1H); MC, m / e 533.90 (M + 1) + 28 4-f-ph H H Me i-pr 1 H NMR (DMSO-d ₆ ) δ 1.13-1.30 (m, 12H), 3.74-3.85 (m, 2H), 3.98-4.06 (m, 1H), 4.234.41 (m, 2H), 4.83-4.87 ( m, 1H), 5.55-5.61 (t, 1H), 5.85-6.12 (m, 3H), 7.18-7.24 (m, 4H), 7.55-758 (d, 1H), 11.50 (s. 1H); MC, m / e 547.91 (M + 1) + 29th 4-f-ph H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.10-1.23 (m, 6H), 3.65-3.89 (m, 3H), 4.10-4.30 (m, 2H), 4.96-5.00 (m, 2H), 5.46-5.50 ( t, 1H), 5.75-5.96 (m, 2H), 6.04-6.12 (m, 1H), 7.05-7.11 (m, 4H), 7.20-7.24 (d, 5H), 7.42-7.45 (d, 1H), 11.50 (s. 1H); MC, m / e 595.94 (M + 1) + thirty 4-MeO-Ph H H Me i-pr 1 H NMR (400 MHz, DMSO-d ₆ ): δ = 1.15-1.27 (m, 1H), 3.71-3.89 (m, 5H), 3.984.02 (m, 1H), 4.22-4.25 (m, 1H) , 4.33-4.39 (m, 1H), 4.84-4.87 (m, 1H), 5.57 (t, J = 12.0 Hz, 1H), 5.91-6.03 (m, 3H), 6.90 (d, J = 8.0 Hz, 2H ), 7.09-7.14 (m, 2H), 7.55 (d, J = 8.0 Hz, 1H), 11.51 (s, 1H) 31 2-Cl-Ph H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.23 (m, 6 H), 3.934.00 (m, 3 H), 4.274.40 (m, 2H), 5.0 (t, J = 7.2 Hz, 2H), 5.53 (m, 1H), 5.80-6.0 (m, 2H), 6.30 (m, 1H), 7.15 (d, J = 2.4 Hz, 1H), 7.27 (m, 6H), 7.51 (m, 3H), 11.5 ( s, 1H); MC, m / e 579.87 (M + 1) + / 596.78 (M + 18) + 32 2,4-Cl-Ph H H Me n-bu 1 H-NMR (DMSO-d ₆ ) δ = 0.82 (m, 3H), 1.23 (m, 8H), 1.47 (m, 2H), 3.86 (m, 2H), 3.84 (m, 3 H), 4.274. 43 (m, 2H), 5.5 (m, 1H), 6.02 (m, 2H), 6.35 (m, 1H), 7.44 (m, 3H), 7.77 (m, 1H), 11.5 (s, 1H); MC, m / e 611.87 (M + 1) + 33 4-Me-Ph H H Me i-pr 1 H NMR (DMSO-d ₆ ) δ 1.14-1.27 (m, 12H), 2.17-2.26 (m, 3H), 3.73-3.82 (m, 1H), 3.994.02 (m, 1H), 4.234.26 ( m, 1H), 4.374.40 (m, 1H), 4.824.88 (m, 1H), 5.52-5.58 (m, 1H), 5.85-6.07 (m, 3H), 7.01-7.20 (m, 4H), 7.55 (d, J = 16 Hz, 1H); 11.51 (s, 1H); MS, m / e 543.98 (M + 1) +; 1108.86 (2M + 23) + 34 4-f-ph H H Me n-bu 1 H-NMR (DMSO-d ₆ ) δ 0.82-0.89 (m, 3H), 1.20-1.31 (m, 8H), 1.48-1.53 (m, 2H), 3.77-3.90 (m, 2H), 3.954.10 ( m, 3H), 4.214.45 (m, 2H), 556-5.61 (t, 1H), 5.83-6.20 (m, 3H), 7.18-7.25 (m, 4H), 7.55-758 (d, 1H), 11.50 (s. 1H); MC, m / e 584.1 (M + 23) + 35 3,4-diCl-Ph H H Me Et 1 H-NMR (DMSO-d ₆ ) δ 1.12-1.31 (m, 9H), 3.77-3.92 (m, 2H), 3.954.08 (m, 3H), 4.214.45 (m, 2H), 5.56-5.62 ( t, 1H), 5.80-6.11 (m, 2H), 6.18-6.33 (m, 1H), 7.18-7.25 (m, 1H), 7.49-7.56 (d, 2H), 7.62-7.67 (m, 1H), 11.50 (s. 1H); MC, m / e 606.1 (M + 23) + 36 2-Cl-Ph H H Me i-pr 1 H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.12-1.16 (m, 6H), 1.21-1.27 (m, 6H), 3.79-3.85 (m, 2H), 4.004.07 (m, 1H) , 4.284.32 (m, 1H), 4.38-4.43 (m, 1H), 4.834.87 (m, 1H), 5.56 (dd, J1 = 16.0 Hz, J = 8.0 Hz, 1H), 5.85-6.12 (m , 2H), 6.20-6.33 (m, 1H), 7.19-7.22 (m, 1H), 7.33 (t, J = 16.0 Hz, 1H), 7.48-755 (m, 3H), 11.55 (s, 1H) 37 4-MeO- H H Me Bn 1 H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.19-1.26 (m, 6H), 3.69-3.70 (s,

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS Ph 3H), 3.87 (m, 2H), 3.99 (m, 1H), 4.20-4.21 (m, 1H), 4.35 (m, 1H), 5.07-5.09 (m, 2H), 554 (t, J = 16.0 Hz . 1H), 5.85-5.92 (m, 1H), 6.04-6.10 (m, 2H), 6.86 (d, J = 8.0 Hz. 2H). 7.09 (dd, J1 = 16.0 Hz, J2 = 4.0 Hz, 2H). 7.30-7.34 (m, 5H). 7.53 (s, 1H), 11.52 (s. 1H) 38 Ph H H Me n-pen 1 H-NMR (DMSO-d ₆ ) δ 0.79-0.81 (m, 3H), 1.17-1.23 (m, 10H), 3.74-3.81 (m. 2H), 3.94-3.96 (m, 3H), 4.19-4.36 ( m, 2H), 5.49-5.54 (m, 1H), 5.87-6.08 (m, 3H), 7.14-7.33 (m, 3H), 7.31-7.35 (m, 2H), 7.51 (d, J = 8 Hz. 1H), 11.51 (s. 1H); MS, m / e 557.9 (M + 1) +; 1136.88 (2M + 23) + 39 4-cl-ph H H Me i-pr 1 H-NMR (DMSO-d ₆ ) δ 1.04-1.19 (m, 12H), 3.76-3.80 (m, 2H), 3.98-4.08 (m, 1H), 4.42-4.42 (m, 2H), 4.82-4.85 ( m, 1H), 5.55-5.60 (m, 1H), 5.80-6.20 (m, 3H), 7.20-7.2 5 (m, 2H), 7.43 (d, J = 8.8 Hz, 1H), 7.54 (d, J = 8 Hz, 1H); 1151 (s, 1H); MS, m / e 563.88 (M + 1) +; 1148.73 (2M + 23) + 40 4-cl-ph H H Me n-bu 1 H-NMR (DMSO-d ₆ ) δ 0.85 (t, J = 7.2 Hz, 3H), 1.22-1.33 (m, 8H), 1.45-1.53 (m, 2H), 3.80-3.87 (m, 2H), 3.96 -4.04 (m, 3H), 4.24-4.27 (m, 1H), 4.35-4.39 (m, 1H), 5.56-5.61 (m, 1H), 5.82-6.11 (m, 2H), 6.15-6.18 (m, 1H), 7.20-756 (m, 4H), 7.51-757 (m. 1H), 1154 (s. 1H); MC, m / e 577.95 (M + 1) + 41 4-cl-ph H H Me Et 1 H NMR (DMSO-d ₆ ) δ 1.14 (t, J = 7.0 Hz, 3H), 1.20-1.28 (m, 6H), 3.77-3.88 (m, 2H), 3.99-4.07 (m, 3H), 4.24 -4.28 (m, 1H), 4.34-4.43 (m, 1H), 5.56-5.61 (m, 1H), 5.86-6.13 (m, 2H), 6.15-6.24 (m, 1H), 7.20-7.26 (m, 2H), 7.44 (d, J = 7.6 Hz, 2H), 7.55 (d, J = 7.6 Hz, 1H), 1155 (s, 1H); MC, m / e 549.11 (M + 1) + 42 4-Me-Ph H H Me n-bu 1 H-NMR (DMSO-d ₆ ) δ 0.79-0.83 (m, 3H), 1.17-1.28 (m, 8H), 1.45-1.47 (m, 2H), 2.22 (d, J = 2.8 Hz, 1H). 3.70-3.90 (m, 2H), 3.95-3.98 (m, 3H), 4.10-4.40 (m, 2H), 551 (t, 1H), 5.80-5.90 (m, 1H), 5.95-6.05 (m, 2H) ), 7.02-7.06 (m, 2H), 7.51 (t, J = 4.2 Hz. 4H), 7.51 (d, 1H), 11.51 (s, 1H); MS, m / e 557.99 (M + 1) +; 1136.84 (2M + 23) + 43 4-me-phe H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.16-1.24 (m, 6H), 2.22 (s, 3H), 3.65-4.03 (m, 3H), 4.11-4.38 (m, 2H), 5.04-5.05 (m, 2H), 5.48-5.50 (m, 1H), 5.77-5.87 (m, 1H), 5.90-6.11 (m, 2H), 6.98-7.10 (m, 4H), 7.28-7.32 (m, 5H), 7.50 ( t, 1H), 11.48 (s, 1H); MC, m / e 592.00 (M + 1) +. 44 Ph H H Et Me 1 H-NMR (DMSO-d ₆ ) δ 0.70-0.80 (m, 3H), 1.11-1.26 (m, 3H), 1.42-1.61 (m, 2H), 3.50-3.54 (m, 3H), 3.58-3.80 ( m, 2H), 3.91-4.02 (m, 1H), 4.12-4.38 (m, 2H), 5.47-5.52 (m, 1H), 5.90-6.03 (m, 2H), 7.08-7.16 (m, 3H), 7.26-7.35 (m, 2H), 7.48 (t, 1H), 11.45 (s, 1H); MS, m / e 515.95 (M + 1) +; 1052.82 (2M + 23) + 45 Ph H H Me 4-F-Bn 1 H NMR (400 MHz, DMSO-d ₆ ): δ 1.20-1.26 (m, 6H), 3.80-3.93 (m, 2H), 3.98 (s, 1H), 4.25-4.26 (m, 1H), 4.36- 4.37 (m, 1H), 5.07 (s, 2H), 552-5.55 (m, 1H), 5.86-5.87 (m, 1H), 5.98-6.04 (m, 1H), 6.14-6.17 (m, 1H), 7.15-7.20 (m, 5H), 7.36 (dd, J = 20.0.8.0 Hz, 4H), 7.54 (s, 1H), 1155 (s, 1H) 46 4-cl-ph H H Me n-bu 1 H-NMR (400 MHz, DMSO-d ₆ ): δ 1.21-1.28 (m, 6H), 3.71-3.88 (m, 1H), 3.91-3.98 (m, 1H), 4.00-4.01 (m, 1H), 4.23-4.27 (m, 1H), 4.35-4.38 (m, 1H), 5.08 (d, J = 4.0 Hz, 2H), 5.57 (dd, J = 12.0, 8.0 Hz, 1H), 5.91 (d, J = 8.0 Hz, 1H), 6.01 (d, J = 8.0 Hz, 1H), 6.22-6.24 (m, 1H),

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 7.17-7.23 (m, 2H), 7.31-7.40 (m, 7H), 7.53 (s, 1H), 11.50 (s, 1H) 47 Ph H H Me 3-Me-1-Bu 1 H-NMR (DMSO-d ₆ ) δ 0.80-0.82 (m, 6H), 1.18-1.40 (m, 8H), 1.50-1.58 (m, 1H), 3.71-3.82 (m, 3H), 3.97-3.4. 01 (m, 3H), 4.21-4.40 (m, 2H), 5.30 (t, J = 8.6 Hz, 1H), 5.81-6.10 (m, 3H), 7.15-7.20 (m, 3H), 7.32-7.36 ( m, 2H), 7.48 (d, J = 8.4 Hz, 1H), 11.38 (s, 1H); MS, m / e 557.98 (M + 1) ⁺ ; 1136.88 (2M + 23) ⁺ 48 3,4-diCl-Ph H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.05-1.37 (m, 6H), 3.71-3.82 (m, 1H), 3.87-4.02 (m, 2H), 4.28-4.29 (m, 1H), 4.36-4.38 ( m, 1H), 5.04 (d, J = 5.2 Hz, 2H), 5.55-5.64 (m, 1H), 5.85-5.94 (m, 1H), 6.00-6.05 (m, 1H), 6.29-6.40 (m, 1H), 7.17-7.24 (m, 1H), 7.30-7.41 (m, 5H), 7.45-7.58 (m, 2H), 7.61 (d, J = 4.0 Hz, 1H), 11.53 (s, 1H); MS, m / e 545.80 (M + 1) ⁺ ; 49 Ph H H Me c-hex 1H-NMR (DMSO-d ₆ ) δ 1.18-1.41 (m, 12H), 1.59-1.67 (m, 4H), 3.74-13.80 (m, 1H), 3.96-4.02 (m, 1H), 4.19-4.26 ( m, 1H), 4.31-4.39 (m, 1H), 4.60 (s, 1H), 552 (t, J = 7.8 Hz, 1H), 5.80-6.09 (m, 3H), 7.15-7.20 (m, 3H) 7.32-7.36 (m, 2H); 7.52 (d, J = 8 Hz, 1H); 11.50 (s, 1H); MS, m / e 569.98 (M + 1) ⁺ ; 592.14 (M + 23) ⁺ fifty Ph H Me H n-bu 1 H-NMR (DMSO-d ₆ ) δ 0.76 (t, J = 7.2 Hz, 3H), 1.10-1.22 (m, 8H), 1.38-1.43 (m, 2H), 3.72-3.75 (m, 2H), 3.87 -3.93 (m, 3H), 4.14-4.21 (m, 1H), 4.23-4.33 (m, 1H), 5.46-5.54 (m, 1H), 5.84-6.11 (m, 3H), 7.09-7.14 (m, 2H), 7.27-7.32 (m, 2H), 7.34-751 (m, 1H), 11.47 (s. 1H); MC, m / e 543.98 (M + 1) ⁺ 51 Ph H Me H i-pr 1 H NMR (DMSO-d ₆ ) δ 1.39 (d, J = 7.2 Hz, 6H), 1.19-1.29 (m, 6H), 3.65-3.75 (m, 2H), 3.95-4.05 (m, 1H), 4.20 -4.22 (m, 1H), 4.31-4.33 (m, 1H), 4.79-4.82 (m, 1H), 5.48-5.57 (m, 1H), 5.84-5.91 (m, 1H), 5.96-6.07 (m, 2H), 7.12-7.35 (m, 5H), 7.44-754 (m. 1H), 11.49 (s, 1H); MC, m / e 529.96 (M + 1) ⁺ 52 Ph H Me H Bn 1H-NMR (DMSO-d ₆ ) δ 1.18-1.28 (m, 6H), 3.70-3.83 (m, 1H), 3.87-3.94 (m, 1H), 3.99-4.01 (m, 1H), 4.23-4.26 ( m, 1H), 4.33-4.37 (m, 1H), 5.03-5.12 (m, 2H), 5.51-559 (m, 1H), 5.87-5.90 (m, 1H), 5.95-6.07, (m, 1H) 6.10-6.27 (m, 1H), 7.15-7.23 (m, 3H), 7.31-7.38 (m, 7H), 7.47-756 (m, 1H), 1150 (s, 1H); MC, m / e 577.99 (M + 1) ⁺ 53 2-Cl-Ph H H Me n-bu 1 H-NMR (400 MHz, DMSO-d ₆ ): δ 0.81-0.86 (m, 3H), 1.21-1.31 (m, 8H), 1.46-1.52 (m, 2H), 3.84-3.90 (m, 2H), 3.97-4.04 (m, 3H), 4.27-4.41 (m, 2H), 553-558 (m, 1H), 5.82-5.95 (m, 1H), 5.96-6.10 (m, 1H), 6.27-6.31 (m , 1H), 7.19-7.22 (m, 1H), 7.34 (dd, J = 8.0.4.0 Hz, 1H), 7.47-755 (m, 3H), 1155 (s, 1H) 54 4-br-ph H H Me i-pr 1 H-NMR (400 MHz, DMSO-d ₆ ): δ 1.10-1.14 (m, 6H), 1.20-1.27 (m, 6H), 3.74-3.81 (m, 2H), 3.99-4.01 (m, 1H), 4.21-4.25 (m, 1H), 4.37-4.38 (m, 1H), 4.81-4.85 (m, 1H), 5.58 (dd, J = 8.0.4.0 Hz, 1H), 5.82-5.95 (m, 1H), 5.96-6.09 (m, 1H), 6.10-6.13 (m, 1H), 7.18 (dd, J = 12.0. 8.0 Hz, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) 55 4-f-ph H H Me c-hex 1 H-NMR (DMSO-d ₆ ) δ 1.20-1.44 (m, 12H), 1.60-1.71 (m, 4H), 3.75-4.02 (m, 2H), 3.94-4.02 (m, 1H), 4.19-4.26 ( m, 2H), 4.59-4.61 (m, 1H), 557 (t, J = 8.4 Hz, 1H), 5.85-6.06 (m, 3H), 7.17-7.23 (m, 4H), 7.54 (d, J = 8.4 Hz, 1H); 11.50 (s, 1H); MC, m / e 587.92 (M + 1) ⁺ 56 4-br-ph H H Me c-hex 1H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.18-1.46 (m, 12H), 1.61-1.69

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS (m, 4H), 3.75-3.82 (m, 2H), 3.95-4.08 (m, 1H), 4.25-4.28 (m, 1H), 4.38 (s, 1H), 4.60-4.62 (m, 1H), 5.56 -5.60 (m, 1H), 5.82-5.95 (m, 1H), 6.02-6.20 (m, 2H), 7.09-7.20 (m, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) MC, m / e 650.0 (M + 3) ⁺ 57 Ph H H Et i-pr 1H-NMR (400 MHz, DMSO-d ₆ ): δ = 0.75-0.82 (m, 3H), 1.12-1.26 (m, 9H), 1.52-1.59 (m. 2H), 3.55-3.68 (m, 1H) , 3.72-3.85 (m, 1H), 3.95-4.08 (m, 1H), 4.18-4.28 (m, 1H), 4.32-4.41 (m, 1H), 4.83-4.86 (m, 1H), 555 (m, J = 7.6 Hz, 1H), 5.99-6.04 (m, 2H), 6.05-6.10 (m, 1H), 7.14-7.21 (m, 3H), 7.33-7.37 (m, 2H), 752-754 (m, 1H), 1153 (s, 1H); MC, m / e 566.07 (M + 23) ⁺ 58 Ph H H Et c-hex 1 H-NMR (400 MHz, DMSO-d ₆ ): δ 0.75-0.88 (m, 3H), 1.26-1.46 (m, 9H), 1.52-1.69 (m, 6H), 3.60-3.63 (m, 1H), 3.72-3.90 (m, 1H), 4.02-4.03 (m, 1H), 4.24-4.27 (m, 1H), 4.37-4.38 (m, 1H), 4.63-4.65 (m, 1H), 5.55 (dd, J = 8.0 G C, 4.4 Hz, 1H), 5.80-5.95 (m, 1H), 6.00-6.07 (m, 2H), 7.15-7.22 (m, 3H), 7.34-7.38 (m, 2H), 754 (d , J = 8.0 Hz, 1H), 1155 (s, 1H); MS, m / e 584.01 (M + 1) ⁺ , 606.17 (M + 23) ⁺ 59 4-f-ph H H Et c-hex 1 H-NMR (DMSO-d ₆ ) δ 0.75-0.84 (m, 3H), 1.24 (d, J = 22.8 Hz, 3H), 1.29-1.47 (m, 6H), 151-1.70 (m, 6H), 3.59 -3.66 (m. 1H), 3.77-3.84 g, (m, 1H), 3.98-4.04 (m, 1H), 4.21-4.27 (m, 1H), 4.34-4.41 (m, 1H), 4.60-4.65 ( m, 1H), 5.56-5.60 (m, 1H), 5.84-5.90 (m, 1H), 6.00-6.08 (m, 2H), 7.20-7.24 (m, 4H), 756 (d, J = 8.0 Hz, 1H), 11.49 (s, 1H); MS, m / e 602.00 (M + 1) ⁺ 60 Ph H H Me F-CH ₂ -CH ₂ - 1 H-NMR (DMSO-d ₆ ) δ 1.18-1.25 (m, 6H), 3.71-3.89 (m, 2H), 3.92-3.99 (m, 1H), 4.19-4.27 (m, 4H), 4.48-4.61 ( m, 2H), 3.94-3.98 (m. 2H), 4.1-4.23 (m, 4H), 5.47-5.52 (m, 1H), 6.01-6.11 (m, 1H), 5.90-6.14, (m, 2H) 7.15-7.21 (m, 3H); 7.32-7.36 (m, 2H); 7.46-7.57 (m, 1H); 11.49 (s, 1H); MC, m / e 533.86 (M + 1) ⁺ 61 Ph H H Me F2CH-
CH ₂ - 1 H-NMR (DMSO-d ₆ ) δ 1.17-1.24 (m, 6H), 3.67-3.81 (m, 1H), 3.89-3.98 (m, 2H), 4.21-4.36 (m, 4H), 5.48-553 ( m, 1H), 5.82-6.05 (m, 2H), 6.18-6.22 (m, 2H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 751 (s, 1H), 1150 ( s, 1H); MS, m / e 551.92 (M + 1) ⁺ ; 62 Ph H H Me (CF ₃ ) ₂ -CH- 1 H-NMR (DMSO-d ₆ ) δ 1.13-1.29 (m, 6H), 3.67-3.81 (m, 1H), 3.94-4.32 (m, 4H), 5.47 (t, J = 8 Hz 1H), 5.82- 6.01 (m, 2H), 6.33-6.36 (m, 1H), 6.70-6.78 (m, 1H), 7.09-7.15 (m, 3H), 7.28-7.32 (m, 2H), 7.43-7.46 (m, 1H) ), 11.44 (s, 1H); MS, m / e 637.90 (M + 1) ⁺ 63 Ph H H Me (CH ₂ F) ₂
-Ch- 1 H-NMR (DMSO-d ₆ ) δ 1.20-1.29 (m, 6H), 3.70-3.90 (m, 1H), 3.91-4.12 (m, 2H), 4.20-4.33 (m, 1H), 4.35-4.48 ( m, 1H), 4.52-4.55 (m, 2H), 4.63-4.67 (m, 2H), 5.20-5.35 (m, 1H), 5.56 (t, J = 8.4 Hz, 1H), 5.80-5.95 (m, 1H), 5.95-6.10 (m, 1H), 6.18-6.21 (m, 1H), 7.18-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.54 (s, 1H), 11.55 (s, 1H); MS, m / e 565.98 (M + 1) ⁺

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 64 Ph H H Me c-Pr-CH ₂ - 1 H NMR (DMSO-d ₆ ) δ 0.20-0.24 (m, 2H), 0.47-0.48 (m, 2H), 0.76-0.84 (m, 3H), 1.03-1.05 (m, 1H), 1.23 (dd, J = 22.4 6.8 Hz 3H), 1.55-1.60 (m, 2H), 3.61-3.68 (m, 1H), 3. 81-3.89 (m, 3H), 3.984.03 (m, 1H), 4.234.29 ( m, 1H), 4.354.41 (m, 1H), 5.56-6.00 (m, 1H), 5.88-5.91 (m, 1H), 6.04-6.10 (m, 2H), 7.20-7.24 (m, 4H). 7.55 (d, J = 7.6 Hz 1H); 11.53 (s, 1H); MC, m / e 573.17 (M + 1) ⁺ 65 Ph H H Et c-pen 1 H NMR (DMSO-d ₆ ) δ 0.75-0.83 (m, 3H), 1.20-1.28 (m, 3H), 1.49-1.63 (m, 8H), 1.76-1.80 (m, 2H), 3.58-3.60 ( m, 1H), 3.70-3.82 (m, 1H), 3.984.05 (m, 1H), 4.24-4.26 (m, 1H), 4.374.42 (m, 1H), 5.03 (s, 1H), 5.54- 5.57 (m, 1H), 5.90-6.00 (m, 1H), 6.02-6.07 (m, 2H), 7.15-7.22 (m, 3H), 7.35-7.39 (m, 2H) 7.55 (d, J = 8, 0 G c, 1H); 11.55 (s, 1H); MC, m / e 570.03 (M + 1) ⁺ Example R ¹¹ R ¹⁰ NMR / MS 67 OH NH ₂ ¹ H-NMR (DMSO-d ₆ ) δ 1.06-1.13 (m, 3H), 1.20-1.24 (m, 3H), 3.27-3.33 (m, 3H), 3.56 (s, 1H), 3.82-3.88 (m , 1H), 4.07-4.13 (m, 1H), 4.25-4.40 (m, 2H), 5.85-5.87 (m, 1H), 5.98-6.09 (m, 2H), 6.59 (s, 32H), 7.14-7.37 (m, 3H), 7.35-7.37 (m, 2H), 7.79 (d, 7 = 7.2 Hz, 1H), 10.69 (s, 1H); MS, m / e 541 (M + 1) ⁺ ; 68 NH ₂ NH ₂ ¹ H-NMR (DMSO-d ₆ ) δ 1.07 (d, 7 = 22.8 Hz, 3H), 1.19 (d, 7 = 7.2 Hz, 3H), 3.51 (s, 3H), 3.62 (s, 1H), 3.75 -3.81 (m, 1H), 4.05-4.11 (m, 1H), 4.27-4.42 (m, 2H), 5.79-5.83 (m, 1H), 5.92 (s, 2H), 6.00-6.09 (m, 2H) 6.75 (s, 2H), 7.08-7.17 (m, 3H), 7.31-7.35 (m, 2H), 7.78 (s, 1H); MS, m / e 540 (M + 1) ⁺ ; 69 NH ₂ c-Pentyl-NH- ¹ H-NMR (DMSO-d ₆ ) δ 1.05 (d, 7 = 22.8 Hz, 3H), 1.09-1.19 (m, 3H), 1.48 (s, 4H), 1.66 (s, 1H), 1.86 (s, 1H), 3.54 (d, 7 = 14 Hz, 3H), 3.65 (s, 1H), 4.25-4.43 (m, 4H), 5.71-5.82 (m, 1H), 5.94-6.04 (m, 4H), 7.11 -7.24 (m, 3H), 7.26-7.34 (m, 2H), 7.77 (d, 7 = 3.6 Hz, 1H); MS, m / e 608 (M + 1) ⁺ 70 NH ₂

¹ H-NMR (DMSO-d ₆ ) δ 1.07 (d, 7 = 22.4 Hz, 3H), 2.35-2.38 (m, 2H), 3.54 (d, 7 = 9.2 Hz, 3H), 3.59-3.62 (m, 2H), 3.65 (s, 1H), 3.75-3.82 (m, 1H), 4.01-4.13 (m, 2H), 4.22-4.40 (m, 6H), 5.75-5.85 (m, 1H), 6.00-6.07 ( m, 4H), 7.15-7.21 (m,

Example R ¹¹ R ¹⁰ NMR / MS 3H), 7.32-7.35 (m, 2H), 7.79 (d, J = 4.0 Hz, 1H); MC, m / e 580 (M + 1) + 71 NH ₂ Et ₂ N- ¹ H-NMR (DMSO-d ₆ ) δ 1.06-1.28 (m, 12H), 3.55 (d, J = 4.8 Hz, 3H), 3.79-3.87 (m, 4H), 4.07-4.12 (m, 2H), 4.29-4.42 (m, 3H), 5.75-5.82 (m, 1H), 5.94 (s, 2H), 6.04-6.10 (m, 2H), 7.14-7.22 (m, 3H), 7.31-7.37 (m, 2H ), 7.82 (d, J = 4.4 Hz, 1H); MC, m / e 596 (M + 1) ⁺ 72 NH ₂ n-Propyl-NH- ¹ H-NMR (DMSO-d ₆ ) δ 0.84 (t, J = 7.2 Hz, 3H), 1.01-1.01 (m, 3H), 1.09-1.12 (m, 3H), 1.51-1.56 (m, 2H), 3.48 (d, f = 15.2 Hz, 3H), 3.79-3.82 (m, 1H), 4.04-4.05 (m, 1H), 4.27-4.38 (m, 3H), 5.72-5.79 (m, 1H), 5.98- 6.04 (m, 4H), 7.13-7.20 (m, 3H), 7.26-7.32 (m, 2H), 7.76 (d, J = 5.2 Hz, 1H); MC, m / e 582 (M + 1) ⁺ 73 NH ₂ c-Butyl-NH- ¹ H-NMR (DMSO-d ₆ ) δ 1.02-1.08 (m, 3H), 1.18 (d, J = 4.8 Hz, 3H), 1.44-1.61 (m, 2H), 2.02-2.17 (m, 4H), 3.51 (d, J = 10.8 Hz, 3H), 3.78-3.83 (m, 1H), 4.03-4.06 (m, 1H), 4.27-4.38 (m, 2H), 4.53-4.62 (m, 1H), 5.68- 5.79 (m, 1H), 5.95-6.04 (m, 4H), 7.11-7.18 (m, 3H), 7.29-7.35 (m, 2H), 7.51-7.58 (m, 1H), 7.78 (d, J = 5.2 Hz, 1H); MC, m / e 594 (M + 1) ⁺ 74 NH ₂

¹ H-NMR (DMSO-d ₆ ) δ 0.97-1.20 (m, 6H), 2.18 (s, 3H), 2.19 (s, 4H), 3.43-3.47 (m, 3H), 3.75 (s, 1H), 4.01-4.06 (m, 4 H), 4.22-4.35 (m, 3H), 5.69-5.75 (m, 1H), 5.98-6.05 (m, 3H), 7.09-7.15 (m, 3H), 7.25-7.29 ( m, 2H), 7.77 (d, J = 3.6 Hz, 1H); MC, m / e 623 (M + 1) ⁺

DOSAGE, INTRODUCTION AND USE

According to a sixth embodiment of the invention, there is provided a composition for treating any viral agent disclosed herein, the aforementioned composition comprises a pharmaceutically acceptable medium selected from an excipient, carrier, solvent and equivalent medium, and a compound contemplating incorporation of its salts (obtained by adding an acid or a base) , hydrates, solvates, and crystalline forms that can be obtained are presented in formula I.

It is contemplated that the wording of the sixth embodiment of the invention may comprise any of the compounds contemplated by any aspect of the first, second, third, fourth, and fifth embodiments of the invention, or certain compounds listed in the tables above or listed here, either individually or in combinations with another compound of the present invention.

Compounds according to the present invention can be obtained in a wide range of forms and carriers for oral administration. Oral administration may be in the form of tablets, coated tablets, hard and soft gelatine capsules, solutions, emulsions, syrups, or suspensions. The compounds of the present invention, among other methods of administration, are effective when administered in the form of suppositories. The most convenient route of administration is usually oral, using a convenient daily dosing regimen that can be adjusted according to the severity of the disease and the patient's sensitivity to antiviral drugs.

The compound or compounds of the present invention, as well as their pharmaceutically acceptable salts, together with one or more commonly used excipients, carriers or solvents, can be formulated into pharmaceutical formulations and unit dosage forms. The pharmaceutical composition and unit dosage forms can be formulated from commonly used ingredients in appropriate proportions with or without the addition of the active compound, and unit dosage forms can contain any suitable effective amount of the active ingredient in accordance with the prescribed daily dosage range. The pharmaceutical compositions can be used in solid forms, such as tablets or filled capsules, semi-solid forms, powders, sustained release dosage forms, or in liquid forms, such as suspensions, emulsions, or in filled capsules for oral administration; or in the form of suppositories for rectal or vaginal administration. A typical drug contains from about 5% to about 95% of the active compound or compounds (w / w). The term “drug” or “dosage form” can mean both solid and liquid dosage forms of the active compound, and one skilled in the art will appreciate that the active ingredient can exist in various dosage forms depending on the desired dose and pharmacokinetic parameters.

The term “excipient”, as used herein, refers to a compound that is used to produce a pharmaceutical composition, and is generally safe, non-toxic, and is not undesirable in a biological or in k / l other sense, including excipients acceptable for veterinary use, as well as for use in human pharmaceuticals. The compounds of the present invention may be administered alone, but will usually be administered with an admixture of one or more suitable pharmaceutical excipients, solvents or carriers in accordance with the intended administration schedule and standard pharmaceutical practice.

The “pharmaceutically acceptable salt” form of the active ingredient may also initially impart desired pharmacokinetic properties to the active ingredient that were not present in the non-salt form, and may even positively affect the pharmacodynamics of the active ingredient with respect to its therapeutic activity in the body. The phrase “pharmaceutically acceptable salt” of a compound as used herein means that the salt is pharmaceutically acceptable and possesses the desired pharmacological activity of the parent compound. Such salts include: (1) salts obtained by the addition of acid formed by inorganic acids such as hydrochloric acid, hydrobromic acid, sulfuric acid, nitrous acid, phosphoric acid, and the like; or formed by organic acids, such as glycolic acid, pyruvic acid, lactic acid, malonic acid, malic acid, maleic acid, fumaric acid, tartaric acid, citric acid, 3- (4-hydroxybenzene) benzoic acid, cinnamic acid, mandelic acid , methanesulfonic acid, ethanesulfonic acid, 1,2-ethane disulfonic acid, 2-hydroxyethanesulfonic acid, benzenesulfonic acid, 4-chlorobenzenesulfonic acid, 2-naphthalenesulfonic acid, 4-toluenesulfonic acid, camphorsulfonic acid, lau yl sulfonic acid, gluconic acid, glutamic acid, salicylic acid, muconic acid, and the like; (2) salts obtained by adding a base formed by bases conjugated to any of the above inorganic acids, where the acid conjugated base contains a cationic component selected from Na ⁺ , K ⁺ , Mg ²⁺ , Ca ²⁺ , and NHgR ^{''_'4-g +,} where ^R''' represents C _1-3 alkyl, and g is an integer selected from 0, 1, 2, 3, or 4. it should be understood that the entire list of pharmaceutically acceptable salts forms includes adding solvent (solvates) or crystalline forms (polymorphs) as defined herein , The same salts obtained by acid addition.

Solid forms of the drug include powders, tablets, pills, capsules, suppositories, and dispersible granules. A solid carrier can be one or more substances, which can also act as solvents, flavoring agents, solubilizers, lubricants, suspending agents, binders, preservatives, disintegrating agents or an encapsulating substance. In powders, the carrier is usually a finely divided solid mixed with a finely divided active component. In tablets, the active ingredient is usually mixed in suitable proportions with a carrier having the necessary binding ability and packaged in the desired shape and size. Suitable carriers include, but are not limited to, magnesium carbonate, magnesium stearate, talc, sugar, lactose, pectin, dextrin, starch, gelatin, tragacanth, methyl cellulose, sodium carboxymethyl cellulose, low melting wax, cocoa butter, and the like. Solid forms of the drug may contain, in addition to the active component, colorants, flavorings, stabilizers, buffers, artificial and natural sweeteners, dispersants, thickeners, solubilizing agents, and the like.

Liquid formulations are also suitable for oral administration, including emulsions, syrups, elixirs, and aqueous suspensions. They include solid forms of the drug intended to be converted to liquid forms immediately before use. Emulsions can be prepared in the form of solutions, for example, in aqueous solutions of propylene glycol, or they can contain emulsifying agents, such as lecithin, sorbitan mono-theater, or gum. Aqueous suspensions can be prepared by dispersing the finely divided active component in water with a viscous substance such as natural gums, resins, methyl cellulose, sodium carboxymethyl cellulose, and other known suspending agents.

The compounds of the present invention may be prepared in the form of suppositories. First, a low melting wax, such as a mixture of fatty acid glycerides or cocoa butter, dissolves and the active ingredient is dispersed homogeneously, for example by agitation. Then the homogeneous liquid mixture is poured into the form of a suitable volume, allow it to cool and harden.

The compounds of the present invention can be formulated for vaginal administration. Uterine rings, tampons, creams, gels, pastes, foams or sprays containing, in addition to the active component, carriers that meet the requirements in this field.

Suitable formulations, together with pharmaceutical excipients, solvents or carriers, are described in Remington: The Science and Practice of Pharmacy 1995, edited by E.W. Martin, Mack Publishing Company, 19th edition, Easton, PA, hereby incorporated by reference. Compounds of the present invention may also be placed on liposomes, such as those shown in US Pat. No. 6,180,134, 5,192,549, 5,376,380, 6,060,080, 6,132,763, the contents of each of which are incorporated herein by reference. One of skill in the art can modify the formulation within the scope of the information provided herein to provide multiple formulations for individual administration regimens without rendering the compounds of the present invention in an unstable state or at risk of deterioration of their therapeutic activity.

The present compounds, in order to achieve their greater solubility in water or another medium, for example, can be easily modified using simple techniques (eg, salt formation), well known to those of ordinary skill in the art. Also, specialists are aware of methods for changing the administration regimen and administration regimen of a particular compound for regulating the pharmacokinetics of the present inventions for maximum therapeutic effect in patients.

According to a seventh embodiment of the present invention, it is proposed to use a compound represented by Formula I for the manufacture of a medicament for the treatment of any condition caused by infection with any of the following viral agents: hepatitis C virus, West Nile fever virus, yellow fever virus, dengue virus, rhinovirus, poliovirus, hepatitis A virus, cattle diarrhea virus, and Japanese encephalitis virus.

The term “drug” or “drug” means an agent used in a method of treating and / or preventing a disease in a patient in need thereof, the above agent includes, but is not limited to, a composition, dosage form, and the like, represented by a compound of formula I It is contemplated that a compound indicated as a compound of formula I in the manufacture of a medicament for the treatment of any viral infectious conditions described herein in a seventh embodiment of the invention may be any of the compounds contemplated by any aspect of the first, second, third, fourth, fifth embodiments, or any of those listed separately in the tables above, or as exemplified herein, either individually or in combination with another compound of the present invention. The drug includes, but is not limited to, any composition contemplated in the sixth embodiment of the invention.

According to an eighth embodiment of the invention, there is provided a method of treating and / or preventing a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound of Formula I.

According to a first aspect of an eighth embodiment of the invention, there is provided a method for treating and / or preventing a patient in need thereof, comprising administering to the patient a therapeutically effective amount of at least two or more compounds falling within the description of the compound represented by formula I.

According to a second aspect of an eighth embodiment of the invention, there is provided a method of treating and / or preventing a patient in need thereof, comprising administering to the patient sequentially or simultaneously a therapeutically effective amount of at least two compounds falling within the description of the compound represented by formula I.

The patient is intended to be a subject in a condition caused by infection with any of the viral agents examined herein, including but not limited to hepatitis C virus, West Nile fever virus, yellow fever virus, dengue virus, rhinovirus, poliovirus, hepatitis A virus, cattle diarrhea virus and Japanese encephalitis virus, flavivirid viruses or pestiviruses, or hepativiruses, or a viral agent, causing symptoms equivalent to or comparable to those caused by any of the above viruses.

The term "patient" means a mammal, including but not limited to cattle, pigs, sheep, chickens, turkey, buffalos, llamas, ostriches, dogs, cats and humans, the preferred patient is a human. It is contemplated that, in a method for treating a patient in need thereof, any of the compounds considered by any aspect of the first, second, and third embodiments, or individually listed in the tables above, alone, or in combination with another compound of the present invention, may be included in a sixth embodiment of the invention .

The term “therapeutically effective amount”, as used herein, means the amount required to reduce the symptoms of a disease in an individual. Dosage is regulated depending on individual needs in each case. Dosage can vary widely depending on several factors, such as the severity of the disease being treated, the patient’s age and general health, other medications the patient is being treated, the regimen and form of administration, as well as the preferences and experience of the practitioner. For oral administration, a suitable dosage for monotherapy and / or combination therapy will be between 0.1 and 10 g, including all intermediate values, such as 0.25, 0.5, 0.75, 1, 1.5, 2, 2.5, 3, 3.5, 4, 4.5, 5 , 5.5, 6, 6.5, 7, 7.5, 8, 8.5, 9, and 9.5 per day. The preferred daily dosage is between 0.5 and 7.5 g per day, the more preferred between 1.5 and 6.0 g per day. Typically, treatment is started with a large initial “saturating dose” to rapidly attenuate or kill the virus, followed by a dose reduction to a level sufficient to prevent the return of infection. The average specialist in the field of infections described here is able, without unnecessary experimental work, relying on their own knowledge, experience and information provided in this description, to establish a therapeutically effective amount of the compounds of the present invention for a particular disease and patient.

Therapeutic efficacy can be established in tests for liver function, including but not limited to: protein levels, for example, serum proteins (e.g. albumin, blood coagulation factors, alkaline phosphatase, aminotransferases (e.g., alanine transaminase, aspartate transaminase) 5 ' -nucleosidase, γ-glutamintranspeptidase, etc.), bilirubin synthesis, cholesterol synthesis, and bile acid synthesis; metabolic function of the liver, including, but not limited to, carbohydrate metabolism, metabolism of amino acids and ammonia. Alternatively, therapeutic efficacy can be measured through the content of HCV RNA. The results of these tests will optimize the dosage.

According to a third aspect of an eighth embodiment of the invention, there is provided a method of treating and / or preventing a patient in need thereof, comprising administering to the patient a therapeutically effective amount of a compound represented by Formula I and a therapeutically effective amount of another antiviral agent, where administration is sequential or simultaneous. It is agreed that the time between consecutive administrations can vary between 1 and 24 hours, which includes any intermediate values, including 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours. Examples of “other antiviral agents” include, but are not limited to, HCV NS3 protease inhibitors (see WO 2008010921, WO 2008010921, EP 1881001, WO 2007015824, WO 2007014925, WO 2007014926, WO 2007014921, WO 2007014920, WO 2007014922, US 2005267018, US 2005267018 , WO 2005037214, WO 2004094452, US 2003187018, WO 200364456, WO 2005028502, and WO 2003006490); HCV NS5B inhibitors (see US 2007275947, US20072759300, WO 2007095269, WO 2007092000, WO 2007076034, WO 200702602, US 2005-98125, WO 2006093801, US 2006166964, WO 2006065590, WO 2006065335, US 2006040882, US 2006040882, US 2006040882, US 2006040882, 2006012078, WO 2005123087, US 2005154056, US 2004229840, WO 2004065367, WO 2004003138, WO 2004002977, WO 2004002944, WO 2004002940, WO 2004000858, WO 2003105770, WO 2003010141, WO 2002057425, WO 200O20206262, US 20060194749, US 20060241064, US 6784166, WO 2007088148, WO 2007039142, WO 2005103045, WO 2007039145, WO 2004096210, and WO 2003037895); HCV NS4 inhibitors (see WO 2007070556 and WO 2005067900); HCV NS5a inhibitors (see US 2006276511, WO 2006120252, WO 2006120251, WO 2006100310, WO 2006035061); Toll-like receptor agonists (see WO 2007093901); and other inhibitors (see WO 2004035571, WO 2004014852, WO 2004014313, WO 2004009020, WO 2003101993, WO 2000006529).

According to a fourth aspect of an eighth embodiment of the invention, there is provided a method for treating a patient in need thereof, comprising administering to the patient sequentially or simultaneously the compound represented by Formula I and another antiviral agent. It is agreed that the time between consecutive administrations can vary between 1 and 24 hours, which includes any intermediate values, including 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours.

According to a fifth aspect of an eighth embodiment of the invention, there is provided a method of treating and / or preventing a patient in need thereof, comprising administering to the patient a therapeutically effective amount of at least one compound represented by Formula I and a therapeutically effective amount of another antiviral agent, where the administration is sequential or at the same time. It is agreed that the time between consecutive administrations can vary between 1 and 24 hours, which includes any intermediate values, including 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours.

According to a sixth aspect of an eighth embodiment of the invention, there is provided a method of treating a patient in need thereof, comprising administering to the patient at least one compound of Formula I and another antiviral agent in series or simultaneously. It is agreed that the time between consecutive administrations can vary between 1 and 24 hours, which includes any intermediate values, including 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, and 23 hours.

Another antiviral agent is believed to include, but is not limited to, interferon-α, interferon-β, pegylated interferon-α, ribavirin, levovirin, viramidine, another nucleoside HCV polymerase inhibitor, non-nucleoside HCV polymerase inhibitor, HCV protease inhibitor, or HCV inhibitor g HCV assembly inhibitor. When an active compound, or a derivative or salt thereof, is administered in combination with another antiviral agent, activity relative to the parent compound may increase. When the treatment is carried out by combination therapy, the administration may be simultaneous or sequential, taking into account such nucleoside derivatives. "Concurrent administration" when used in the present description means the introduction of agents at the same time, or at different times. The introduction of two or more agents at the same time can be carried out in a single formulation containing two or more active ingredients, or by almost simultaneous administration of two or more dosage forms with one active component.

It will become clear that the mention of treatment in the present description extends to prevention as well as to treatment of existing conditions. Moreover, the term “treating” HCV infection as used herein also includes the treatment or prophylaxis of a disease or condition associated with or mediated by HCV infection or clinical symptoms of the above infection.

METHOD FOR PRODUCING

According to a ninth embodiment of the present invention, there is provided a process for preparing a compound of formula I, comprising reacting a phosphochloride containing suitable substituents of formula 4 with a nucleoside analog of formula 5

where the substituents R ¹ , R ² , R ^3a , R ^3b , R ⁴ , R ⁵ , X, Y, R ⁶ and the base (base) have the meanings corresponding to those described in the Detailed Description of the Invention, and X 'represents a leaving group, such such as Cl, Br, I, tosylate, mesylate, trifluoroacetate, trifluorosulfonate, pentafluorophenoxide, p-NO ₂ -phenoxide, or another commonly used leaving group as described in Advanced Organic Chemistry by March, Fourth Edition. Leaving groups and methods that can be used in the process of forming a phosphoramidate nucleoside conjugate can be found in US 20060142238 and WO 2007095269. Preferably, the leaving group is Cl.

The reaction is carried out in a non-aqueous aprotic solvent, such as tetrahydrofuran, dioxane, or tetrahydrofuran and dioxane together, or any functional equivalent thereof, tetrahydrofuran is the preferred solvent. Typically, the reaction is carried out at a temperature of from -78 ° C to 40 ° C, the preferred reaction temperature is between 0 ° C and room temperature. First, the nucleoside is mixed with a base (5 to 12 equivalents), such as N-methylimidazole, collidine, pyridine, 2,6-lutidine, 2, 6- ^t Bu-pyridine, etc. a basic tertiary amine, such as triethylamine, diisopropylethylamine, etc., or a Grignard alkyl reagent, such as tBuMgCl, tBuMgBr, MeMgCl, MeMgBr, etc. Phosphochloride (3-10 equivalents) is diluted in the reaction solvent and added to the mixture of nucleoside and base. The reactions are then allowed to proceed at a temperature between room temperature and 40 *** C for a period of time from 30 minutes to 24 hours, the preferred temperature is room temperature, the preferred time is 24 hours. The solvent is removed from the reaction mixture and the reaction product is purified by silica gel chromatography .

According to a tenth embodiment of the present invention, there is provided a product obtained by a process comprising reacting a phosphochloride containing suitable substituents of formula 4 with a nucleoside analogue of formula 5

where the substituents R ¹ , R ² , R ^3a , R ^3b , R ⁴ , R ⁵ , X, Y, R ⁶ , X 'and the base (base) have the meanings corresponding to those described in the Detailed Description of the Invention.

The reaction can be carried out in a non-aqueous aprotic solvent such as tetrahydrofuran, dioxane, or a mixture of tetrahydrofuran and dioxane, tetrahydrofuran is the preferred solvent. Typically, the reaction is carried out at a temperature of from -78 ° C to 40 ° C, the preferred reaction temperature is between 0 ° C and room temperature. The nucleoside is first mixed with a base (5 to 12 equivalents), such as N-methylimidazole, basic tertiary amine or t-magnesium butyl chloride. Phosphochloride (3-10 equivalents, or a suitable phospho (leaving group) value) is diluted in the reaction solvent and added to the mixture of nucleoside and base. The reactions are then allowed to proceed at a temperature between room temperature and 40 ° C. for a period of time from 30 minutes to 24 hours, the preferred temperature is room temperature, the preferred time is 24 hours. The solvent is removed from the reaction mixture and the reaction product is purified by silica gel chromatography.

COMPOUNDS AND RECEIPT

The phosphoramidate compounds of the present invention can be prepared by condensing a nucleoside analog 5 with a phosphochloride compound containing suitable substituents 4 (Scheme 1). The nucleoside analogue is created by standard procedures described in any of the U.S. Published Application Nos. 2005/0009737, 2006/0199783, 2006/0122146, and 2007/0197463, each of which is hereby incorporated by reference and in its entirety.

The set values of 1H-NMR were recorded on a Varian AS-400 instrument. Mass spectral analysis data was obtained using the Micromass-Quattromicro API or Waters Acquity.

So, by way of example only, phenol containing suitable substituents can react with phosphorus oxychloride 1 to form aryloxy phosphodichloride 2 (see Example 1), which is then acted upon with the acid addition salt of the α-amino acid ester in the presence of TEA to form phosphochloride 4. This arylalkoxy amino acid phosphoramidate is reacted with a nucleoside analog to obtain product I (for the procedure, see, for example, C. McGuigan et al. Antiviral Res. 1992 17: 311-321; D. Curley et al. Antiviral Res. 1990 14 : 345-356; McGuigan et al. Antiviral Chem. Chemother 1990 1 (2): 107-113).

The preparation of nucleoside phosphoramidates requires the interaction of a phosphochloride containing suitable substituents with a nucleoside having a free 5′-hydroxyl functional group. In cases where only one hydroxyl group is present, the production of phosphoramidate is usually carried out directly when the phosphochloride reacts with the desired nucleoside. In cases where a nucleoside contains more than one free hydroxyl group, the preparation of a suitably protected nucleoside may be required. Silyl, acetonide, or other alcohol protecting groups known in the art can be used to protect the saccharide functional group. An amidine protection strategy may be required to protect the nucleoside base protecting the free amino group.

Phosphochloride condensation can be carried out on an unprotected nucleoside. Since the 5’-OH group is much less spatially closed than the 3’-OH group, selective phosphoramidation is possible under carefully controlled conditions. After condensation to form a protected nucleoside phosphoramidate, in order to obtain free nucleoside phosphoramidate, deprotection can be carried out using standard nucleic acid chemistry protocols. In many cases, the desired product is easily separated from the starting material using silica gel chromatography. A generalized synthesis scheme is shown in Scheme 1.

A further concept of the above embodiments of the invention can be achieved by considering the following examples, intended only as illustrative but not exhaustive of the present invention.

EXAMPLE 1

The Main Method of Producing Phosphodichlorides

A solution of the corresponding phenol R ¹ —OH (1 eq) and triethylamine (1 eq) in anhydrous ether was added dropwise to a stirred solution of phosphorus trichloride 1 (1 eq) at 0 ° C for three hours under nitrogen. Then the temperature was raised to room temperature, and the reaction mixture was stirred overnight. The triethylamine salt was quickly removed by suction filtration, and the filtrate was concentrated in vacuo to dryness to give 2 in the form of an oil, which was used without further purification.

EXAMPLE 2

The Basic Method for the Preparation of Phosphochlorides

A solution of triethylamine (2 equiv) in anhydrous dichloromethane was added dropwise to a solution of aryloxy phosphodichloride 2 (1 equiv) and the corresponding amine ester 3 (1 equiv) in anhydrous dichloromethane with vigorous stirring at -78 ° C for a period from 30 to 120 minutes. Then the temperature was raised to room temperature, and the reaction mixture was stirred overnight. The solvent was removed. The residue was washed with ethyl ether and filtered, and the filtrate was dried under reduced pressure to obtain 4.

EXAMPLE 3

Basic Methods for the Preparation of Nucleoside Phosphoramidate Derivatives

A solution of the corresponding phosphochloride 4 (6.5 equivalents) in anhydrous tetrahydrofuran (THF) was added to a mixture of nucleoside 5 (1 equivalent) and N-methylimidazole (8 equivalents) in anhydrous THF with vigorous stirring at room temperature, and the reaction mixture was stirred overnight . The solvent was removed in vacuo, and the distillate was purified by column chromatography and / or preparative thin layer chromatography to obtain I.

EXAMPLE 4

Preparation of 2’-deoxy-2’-fluoro-2’-C-methyluridine

2'-deoxy-2'-fluoro-2'-C-methylcytidine (1.0 g, 1 equivalent) (Clark, J., et al., J. Med. Chem., 2005, 48, 5504-5508) were bred 10 ml of anhydrous pyridine and concentrated in vacuo. The resulting syrup was diluted in 20 ml of anhydrous pyridine under nitrogen and cooled to 0 ° C with stirring. The brown solution was treated with benzoyl chloride (1.63 g, 3 equiv) dropwise for 10 minutes. The ice bath was removed and stirring; lasted for 1.5 h, as a result of which thin-layer chromatography (TLC) showed that no starting material remained. The mixture was sharply cooled by adding water (0.5 ml) and concentrated to dryness. The precipitate was dissolved in 50 ml of dichloromethane (DCM) and washed with saturated aqueous NaHCO ₃ and H ₂ O. The organic phase was dried over NaSO ₄ and filtered, concentrated to dryness to give N ⁴ , 3 ', 5'-tribenzoyl-2'-deoxy- 2'-fluoro-2'-C-methylcytidine (2.0 g, yield: 91%).

N ⁴ , 3 ', 5'-tribenzoyl-2'-deoxy-2'-fluoro-2'-C-methylcytidine (2.0 g, 1 equivalent) was refluxed in 80% aqueous AcOH overnight. After cooling and placing at room temperature (15 ° C), most of the product precipitated, after which it was filtered through a filter funnel. The white precipitate was washed with water and co-evaporated with toluene to obtain a white solid. The filtrate was concentrated and co-evaporated with toluene to obtain an additional product, which was washed with water to obtain a white solid. By combining two portions of a white solid, 1.50 g of 3 ', 5'-tribenzoyl-2'-deoxy-2'-fluoro-2'-C-methyluridine was obtained (yield: 91%).

To a solution of 3 ’, 5’-tribenzoyl-2’-deoxy-2’-fluoro-2’-C-methyluridine (1.5 g, 1 equiv) in MeOH (10 ml) was added a solution of saturated ammonia in MeOH (20 ml). The reaction mixture was stirred at 0 ° C for 30 minutes, and then slowly warmed to room temperature. After stirring for 18 h, the reaction mixture was evaporated under reduced pressure to obtain a residue, which was purified by column chromatography to obtain pure 2’-deoxy-2’-fluoro-2’-C-methyluridine (500 mg, 60% yield).

EXAMPLE 5

Preparation of 2’-deoxy-2’-fluoro-2’-C-methyluridine 5 ’- (phenyl methoxy alanyl phosphate)

Phenyl methoxyalanyl phosphochloride (1 g, 6.5 equiv) diluted in 3 ml of THF was added to a mixture of 2'-deoxy-2'-fluoro-2'-C-methyluridine (0.15 g, 1 equiv) and N-methylimidazole (0.3 g , 8 eq) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (50.1 mg, 15.6%). ¹ N NMR (DMSO-d ₆ ) δ 1.20-1.27 (m, 6Н), 3.58 (d, J = 16.0 Hz, 3Н), 3.75-3.92 (m, 2Н), 4.015-4.379 (m, 2Н), 5.54 (t, J = 10.2 Hz, 1H), 5.83-5.91 (m, 1H), 6.00-6.16 (m, 1H), 7.18 (d, J = 8.0 Hz, 2H), 7.22 (s, 1H), 7.35 ( t, J = 4.4 Hz, 2H), 7.55 (s, 1H), 11.52 (s, 1H); MS, m / e 502 (M + 1) ⁺ .

EXAMPLE 6

Preparation of 2’-deoxy-2’-fluoro-2’-C-methyluridine 5 ’- (phenyl methoxy-valyl phosphate)

Phenyl methoxy valyl (0.6 g, 3.6 equiv) diluted in 3 ml of THF was added to a mixture of 2'-deoxy-2'-fluoro-2'-C-methyluridine (0.15 g, 1 equiv) and N-methylimidazole (0.44 g, 9 eq) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (60 mg, 20%). ¹ H NMR (DMSO-d ₆ ) δ 0.74-0.847 (m, 6H), 1.20-1.28 (m, 3H), 1.89-1.92 (m, 1H), 3.50-3.54 (m, 1H), 3.58 (d, J = 10.4Hz, 3H), 3.72-3.95 (m, 1H), 4.03-4.05 (m, 1H), 4.23-4.43 (m, 2H), 5.56 (t, 7 = 16.0 Hz, 1H), 5.85-5.92 (m, 1H), 6.01-6.07 (m, 1H), 7.16-7.21 (m, 3H), 7.37 (t, J = 8 Hz, 2H), 7.55-7.60 (m, 1H), 11.52 (s, 1H ); MS, m / e 530 (M + 1) ⁺ .

EXAMPLE 7

Preparation of 2’-deoxy-2’-fluoro-2’-C-methyluridine 5 ’- (4-bromophenyl methoxy-valyl phosphate)

4-bromophenyl methoxy-valyl phosphochloride (1 g, 3.4 eq) diluted in 3 ml of THF was added to a mixture of 2'-deoxy-2, -fluoro-2'-C-methyluridine (0.2 g, 1 eq) and N- methylimidazole (0.35 g, 6 equiv) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (120 mg, 26%). ¹ H NMR (DMSO-4) δ 0.72-0.82 (m, 6H), 1.19-1.26 (m, 3H), 1.86-1.92 (m, 1H), 3.48-3.50 (m, 1H), 3.56 (d, J = 12.0 Hz, 3H), 3.72-3.89 (m, 1H), 3.96-4.03 (m, 1H), 4.22-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.85-5.91 (m, 1H ), 5.98-6.13 (m, 1H), 7.15 (d, J = 8.0 Hz, 2H), 7.49-7.56 (m, 3H), 11.53 (s, 1H); MS, m / e 608 (M + 1) ⁺ .

EXAMPLE 8

Preparation of 2’-deoxy-2’-fluoro-2’-C-methyluridine 5 ’- (4-bromophenyl methoxy-alanyl phosphate)

4-bromophenyl methoxy-alanyl phosphochloride (0.6 g, 5 equiv) diluted in 3 ml of THF was added to a mixture of 2'-deoxy-2'-fluoro-2'-C-methyluridine (0.25 g, 1 equiv) and N- methylimidazole (0.3 g, 7.8 eq) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (40 mg, 12%); ¹ H NMR (DMSO-d ₆ ) δ 1.20-1.26 (m, 6H), 3.57 (d, J = 2.8 Hz, 3H), 3.84 (s, 1H), 3.97-4.03 (m, 1H), 4.21-4.25 (m, 1H), 4.33-4.37 (m, 2H), 5.54-5.60 (m, 1H), 5.83-5.89 (m, 1H), 5.98-6.19 (m, 1H), 7.16 (t, J = 10.2 Hz , 2H), 7.52-7.57 (m, 3H), 11.52 (s, 1H); MS, m / e 580 (M + 1) ^+.

EXAMPLE 9

Obtaining N ⁴ - (N, N-dimethylphosphamidinyl) -2'-deoxy-2, -fluoro-2'-C-methylcytidine

2’-deoxy-2’-fluoro-2’-C-methylcytidine (500 mg, 1.9 mmol) was mixed with dimethylformamide dimethyl acetal in DMF (10 ml). The resulting mixture was stirred at room temperature overnight. After removing the solvent, the crude product was used in the next step without purification.

EXAMPLE 10

Preparation of 2’-deoxy-2’-fluoro-2’-C-methylcytidine 5 ’- (phenyl methoxy-alanyl phosphate)

Phenyl methoxyalanyl phosphochloride (0.6 g, 6 eq.), Diluted in 3 ml THF, was added to a mixture of N ⁴ - (N, N-dimethylformamidinyl) -2'-deoxy-2'-fluoro-2'-C-methylcytidine (0.15 g , 1 equiv) and N-methylimidazole (0.3 g, 7.8 equiv) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (62 mg, 20.6%). ¹ N NMR (DMSO-d ₆ ) δ 1.16 (d, J = 23.2 Hz, 3H), 1.22 (d, J = 7.2 Hz, 3H), 3.56 (S, 3H), 3.69-3.75 (d, J = 25.6 Hz, 1H), 3.82-3.86 (m, 1H), 3.96-3.98 (m, 1H), 4.21-4.34 (m, 2H), 5.68 (d, J = 7.2 Hz, 1H), 5.75-5.77 (m, 1H), 6.07-6.16 (m, 1H), 7.15-7.19 (m, 3H), 7.2 (d, J = 9.2 Hz, 2H), 7.39 (t, J = 7.8 Hz, 2H), 7.48 (d, J = 9.2 Hz, 1H); MS, m / e 501 (M + 1) ⁺ .

EXAMPLE 11

Preparation of 2’-deoxy-2’-fluoro-2’-C-methylcytidine 5 ’- (4-bromophenyl methoxy-valyl phosphate)

4-bromophenyl methoxy-valyl phosphochloride (1 g, 3.4 equiv), diluted in 3 ml of THF, was added to a mixture of N ⁴ - (N, N-dimethylformamidinyl) -2'-deoxy-2'-fluoro-2'-C- methylcytidine (0.2 g, 1 equiv) and N-methylimidazole (0.35 g, 6 equiv) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (59 mg, 13%); ¹ H NMR (DMSO-d ₆ ) δ 0.74-0.83 (m, 6H), 1.12-1.20 (m, 3H), 1.89-1.92 (m, 1H), 3.49-3.51 (m, 1H), 3.55 (s, 3H), 3.59-3.68 (m, 1H), 3.72-.383 (m, 1H), 4.21-4.39 (m, 2H), 5.70-5.72 (m, 1H), 5.76-5.83 (m, 1H), 6.04 -6.16 (m, 1H), 7.15 (d, J = 13.0 Hz, 2H), 7.26 (s, 1H), 7.33 (s, 1H), 7.46-7.55 (m, 1H), 7.56 (d, J = 4.4 Hz, 2H); MS, m / e 607 (M + 1) ⁺ .

EXAMPLE 12

Preparation of 2’-deoxy-2’-fluoro-2’-C-methylcytidine 5 ’- (phenyl methoxy-valyl phosphate)

Phenyl methoxy-valyl phosphochloride (0.6 g, 6 equiv) diluted in 3 ml of THF was added to a mixture of N ⁴ - (N, N-dimethylformamidinyl) -2'-deoxy-2'-fluoro-2'-C-methylcytidine ( 0.15 g, 1 equiv) and N-methylimidazole (0.3 g, 7.8 equiv) in 3 ml of THF with vigorous stirring at room temperature, after which the reaction mixture was stirred overnight. The solvent was removed under reduced pressure. The resulting crude product was dissolved in methanol purified by prep-HPLC on a YMC 25 × 30X2 mm column using a water / acetonitrile gradient washable mobile phase. Acetonitrile and water were removed under reduced pressure to obtain the desired product (86 mg, 42.9%). ¹ H NMR (DMSO-d ₆ ) δ 0.72-0.80 (m, 6H), 1.09-1.18 (m, 3H), 1.87-1.92 (m, 1H), 3.47-3.51 (m, 1H), 3.58 (s, 3H), 3.71-3.75 (m, 1H), 3.97 (t, J = 11.2 Hz, 1H), 4.22-4.37 (m, 2H), 5.70 (d, J = 8.0 Hz, 1H), 5.76-5.84 (m , 1H), 6.01-6.15 (m, 1H), 7.13-7.18 (m, 3H), 7.27 (s, 2H), 7.34 (d, J = 4.0 Hz, 2H), 7.46-7.50 (m, 1H); MS, m / e 529 (M + 1) ⁺ .

EXAMPLES

Compounds according to Examples numbered 13-54 and 56-66 were obtained using the same techniques as described for examples 5-8. Example number, connection features, and NMR / MS data are shown below:

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 13 Ph H H Me Et 1H-NMR (DMSO-d ₆ ) δ 1.12-1.16 (m, 3H), 1.20-1.28 (m, 6H), 3.70-3.90 (m, 2H), 4.00-4.08 (m, 3H), 4.18-4.45 ( m, 2H), 5.52-5.58 (m, 1H), 5.85-5.98 (m, 1H), 6.00-6.20 (m, 2H), 7.16-7.23 (m, 3H), 7.37-7.40 (m, 2H), 7.54-7.60 (m, 1H); 11.54 (s. 1H); MC, m / e 516.1 (M + 1) + fourteen 1-napth H H Me Bn 1H-NMR (DMSO-d ₆ ) δ 1.18-1.30 (m, 6H), 3.784.10 (m, 3H), 4.38-4.49 (m, 2H), 4.99-5.11 (m, 2H), 5.28-5.40 ( m, 1H), 5.85-6.10 (m. 2H), 6.30-6.41 (m, 1H), 7.28-7.32 (m, 5H), 7.41-7.60 (m, 5H), 7.73-7.76 (m, 1H), 7.94-8.11 (m, 1H), 8.13-8.15 (m, 1H), 11.50 (s. 1H); MC, m / e 628.4 (M + 1) + fifteen Ph H H H Me 1H-NMR (DMSO-d ₆ ) δ 1.22 (d, J = 22.4 Hz. 3H), 3.59 (s, 3H), 3.63-3.69 (m, 2H), 3.74-3.8 (m, 1H), 4.02 (d , J = 11.2 Hz. 1H). 4.23-4.28 (m, 1H), 4.404.43 (m, 1H), 5.57-5.60 (m, 1H), 5.89 (d. J = 6.8 Hz, 1H), 6.00-6.06 (m, 2H), 7.15- 7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.52 (d, J = 8 Hz, 1H), 11.52 (s, 1H); MC, m / e 487.97 (M + 1) +

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 16 2,4-Cl-Ph H H Me Me 1H-NMR (DMSO-d ₆ ) δ 1.22-1.28 (m, 6H), 3.57-3.60 (m, 3H), 3.84-3.92 (m, 2H), 4.00-4.04 (m. 1H). 4.31-4.44 (m, 2H), 5.54-5.61 (m, 1H), 5.85-6.10 (m, 2H), 6.32-6.43 (m, 1H), 7.44-7.54 (m, 3H), 7.72-7.75 (m . 1H), 11.54 (s. 1H); MC, m / e 570.2 (M + 1) + 17 1-napth H H Me Me 1H-NMR (DMSO-d ₆ ) δ 1.15-1.27 (m, 6H), 3.51-3.55 (d, 3H), 3.85-3.96 (m, 2H), 4.00-4.10 (m, 1H), 4.30-4.46 ( m, 2H), 5.31-5.39 (m, 1H), 5.89-6.05 (m, 2H), 6.22-6.34 (m, 1H), 7.44-7.60 (m, 5H). 7.73-7.77 (m, 1H), 7.93-7.96 (m, 1H), 8.12-8.14 (m, 1H) .11.50 (s.1H); MC. m / e 552.1 (M + 1) + eighteen Ph H * Me 1 H NMR (DMSO-d ₆ ) δ 1.19 (d. J = 22.8 Hz. 3H), 1.69-1.84 (m, 3H). 1.99-2.04 (m, 1H), 3.16-3.21 (m, 2H), 3.58 (s, 3H), 3.68-3.8 (m, 1H), 4.00 (m, 1H), 4.01-4.13 (m, 1H), 4.22-4.25 (m, 1 H), 4.5 (d, J = 11.2 Hz, 1H), 5.54 (d, J = 8.0 Hz, 1H), 5.86 (s, 1H), 5.6 (d, J = 19.6 Hz, 1H), 7.15-7.2 (m, 3H), 7.34 (t, J = 8.0 Hz, 2H), 7.51 (d. J = 8.0 Hz, 1H), 11.38 (s, 1H); MC, m / e 527.93 (M + 1) + 19 Ph H H Me n-bu 1H-NMR (DMSO-d ₆₎ δ 0.80-0.90 (m, 3H) , 1.20-1.35 (m, 8H), 1.48-155 (m, 2H), 3.78-3.88 (m, 2H), 3.95-4.08 ( m, 3H), 4.22-4.45 (m, 2H), 555-557 (t, 1H), 5.85-6.18 (m, 3H), 7.14-7.23 (m, 3H), 7.35-7.40 (m, 2H), 7.51-7.60 (d, 1H), 1150 (s.lH); MC, m / e 544.2 (M + 1) + twenty Ph H H Me Bn 1 H-NMR (DMSO-d ₆ ) δ 1.20-1.30 (m, 6H), 3.72-4.05 (m, 3H), 4.23-4.27 (m, 1H), 4.32-4.45 (m, 1H), 5.07-5.10 ( t, 2H), 5.52-5.56 (1, 1H), 5.86-6.10 (m, 2H), 6.13-6.21 (m, 1H), 7.15-7.21 (m, 3H), 7.29-7.40 (m, 7H), 7.51-7.56 (d, 1H), 11.50 (s. 1H); MC, m / e 578.2 (M + 1) + 21 4-f-ph H H Me Me 1H-NMR (DMSO-d ₆₎ δ 1.28-1.34 (m, 6H) , 3.65 (d, J = 4Hz, 3H), 3.85-3.96 (m, 2H), 4.06-4.12 (m, 1H), 4.30 -4.34 (m, 1H), 4.40-4.47 (m, 1H), 5.62-5.67 (m, 1H), 5.94-6.01 (m, 1H), 6.09 (d, J = 18.8 Hz, 1H), 6.17-6.26 (m, 1H), 7.27-7.33 (m, 4H), 7.62 (d, J = 7.6 Hz, 1H), 11.61 (s, 1H); MC, m / e 519.94 (M + 1) + 22 4-cl-ph H H Me Me 1 H-NMR (DMSO-d ₆ ) δ 1.22-1.28 (m, 6H), 358 (d, 2H), 3.70-3.95 (m, 2H), 3.95-4.08 (m, 1H), 4.23-4.45 (m, 2H), 5.55-5.61 (t, 1H), 5.85-6.10 (m, 2H), 6.15-6.23 (m, 1H), 7.20-7.26 (m, 2H), 7.43-7.46 (m, 2H), 7.54- 757 (d, 1H); 11.50 (s. 1H); MC, m / e 536.1 (M + 1) + 23 3,4-Cl-Ph H H Me Me 1H-NMR (DMSO-d ₆ ) δ 1.13 (m, 6H), 3.49 (s, 3H), 3.61-3.85 (m, 2H), 3.90-3.93 (m, 1H), 4.16-4.22 (m, 1H) , 4.27-4.31 (m, 1H), 5.47-5.52 (m, 1H), 5.82 (d, J = 11.6 Hz, 1H), 5.93 (d, J = 19.2 Hz, 1H), 6.15-6.25 (m, 1H ), 7.13 (t, J = 9.6 Hz, 1H), 7.43 (d, J = 12 Hz, 2H), 757 (d, J = 6.0 Hz, 1H), 11.43 (s, 1H); MC, m / e 569.85 (M + 1) + 24 Ph H H Me 2-bu 1H-NMR (DMSO-d ₆ ) δ 0.83 (d, J = 6.8 Hz, 6H), 1.20-1.26 (m, 6H), 1.79-1.86 (m, 1H), 3.73-3.90 (m, 4H), 4.01 (t, J = 11.2 Hz, 1H), 4.21-4.28 (m, 1H), 4.33-4.42 (m, 1H), 5.54 (t, J = 7.6 Hz, 1H), 5.85-5.92 (m, 1H), 5.99-6.13 (m, 2H), 7.19 (t, J = 8 Hz, 3H), 7.36 (t, J = 7.6 Hz, 2H), 7.53 (d, J = 7.6 Hz, 1H), 11.52 (s, 1H ); MC, m / e 544.00 (M + 1) + 25 Ph H H Me i-pr 1H-NMR (DMSO-d ₆ ) δ 1.13-1.28 (m, 12H), 3.74-3.81 (m, 2H), 3.95-4.08 (m, 1H), 4.20-4.45 (m, 2H), 4.83-4.87 ( m, 1H), 5.52-558 (m, 1H), 5.84-6.15 (m, 3H), 7.17-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.54-7.57 (m, 1H), 1150 (s. 1H); MC, m / e 530.2 (M + 1) +

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 26 4-MeO-Ph H H Me n-bu 1H-NMR (400 MHz, DMSO-d ₆ ): δ = 0.78-0.82 (m, 3H), 1.29-1.47 (m, 8H), 1.49-1.54 (m, 2H), 3.66-3.87 (m, 5H) , 3.96-4.02 (m, 3H), 4.21-4.39 (m, 2H), 557 (t, J = 12.0 Hz, 1H), 5.84-6.05 (m, 3H), 6.90 (dd, J1 = 8.0 Hz, J4 = 4.0 Hz, 2H), 7.09-7.14 (dd, J1 = 16.0 Hz, 12 = 4.0 Hz, 2H), 7.55 (d, J = 8.0 Hz, 1H), 11.48-11.62 (s, 1H) 27 4-f-ph H H Me Et 1H-NMR (DMSO-d ₆ ) δ 1.12-1.28 (m, 9H), 3.72-3.94 (m, 2H), 3.98-4.10 (m, 3H), 4.214.42 (m, 2H), 5.55-5.61 ( t, 1H), 5.85-6.20 (m, 3H), 7.18-7.25 (m, 4H), 7.55-7.58 (d, 1H), 11.50 (s. 1H); MC, m / e 533.90 (M + 1) + 28 4-f-ph H H Me i-pr 1H-NMR (DMSO-d ₆ ) δ 1.13-1.30 (m, 12H), 3.74-3.85 (m, 2H), 3.98-4.06 (m, 1H), 4.234.41 (m, 2H), 4.83-4.87 ( m, 1H), 5.55-5.61 (t, 1H), 5.85-6.12 (m, 3H), 7.18-7.24 (m, 4H), 7.55-758 (d, 1H), 11.50 (s. 1H); MC, m / e 547.91 (M + 1) + 29th 4-f-ph H H Me Bn 1H-NMR (DMSO-d ₆ ) δ 1.10-1.23 (m, 6H), 3.65-3.89 (m, 3H), 4.10-4.30 (m, 2H), 4.96-5.00 (m, 2H), 5.46-5.50 ( t, 1H), 5.75-5.96 (m, 2H), 6.04-6.12 (m, 1H), 7.05-7.11 (m, 4H), 7.20-7.24 (d, 5H), 7.42-7.45 (d, 1H), 11.50 (s. 1H); MC, m / e 595.94 (M + 1) + thirty 4-MeO-Ph H H Me i-pr 1H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.15-1.27 (m, 1H), 3.71-3.89 (m, 5H), 3.984.02 (m, 1H), 4.22-4.25 (m, 1H) , 4.33-4.39 (m, 1H), 4.84-4.87 (m, 1H), 5.57 (t, J = 12.0 Hz, 1H), 5.91-6.03 (m, 3H), 6.90 (d, J = 8.0 Hz, 2H ), 7.09-7.14 (m, 2H), 7.55 (d, J = 8.0 Hz, 1H), 11.51 (s, 1H) 31 2-Cl-Ph H H Me Bn 1H-NMR (DMSO-d ₆ ) δ 1.23 (m, 6 H), 3.934.00 (m, 3 H), 4.274.40 (m, 2H), 5.0 (t, J = 7.2 Hz, 2H), 5.53 (m, 1H), 5.80-6.0 (m, 2H), 6.30 (m, 1H), 7.15 (d, J = 2.4 Hz, 1H), 7.27 (m, 6H), 7.51 (m, 3H), 11.5 ( s, 1H); MC, m / e 579.87 (M + 1) + / 596.78 (M + 18) + 32 2,4-Cl-Ph H H Me n-bu 1H-NMR (DMSO-d ₆ ) δ = 0.82 (m, 3H), 1.23 (m, 8H), 1.47 (m, 2H), 3.86 (m, 2H), 3.84 (m, 3 H), 4.274. 43 (m, 2H), 5.5 (m, 1H), 6.02 (m, 2H), 6.35 (m, 1H), 7.44 (m, 3H), 7.77 (m, 1H), 11.5 (s, 1H); MC, m / e 611.87 (M + 1) + 33 4-Me-Ph H H Me i-pr 1H-NMR (DMSO-d ₆ ) δ 1.14-1.27 (m, 12H), 2.17-2.26 (m, 3H), 3.73-3.82 (m, 1H), 3.994.02 (m, 1H), 4.234.26 ( m, 1H), 4.374.40 (m, 1H), 4.824.88 (m, 1H), 5.52-5.58 (m, 1H), 5.85-6.07 (m, 3H), 7.01-7.20 (m, 4H), 7.55 (d, J = 16 Hz, 1H); 11.51 (s, 1H); MS, m / e 543.98 (M + 1) +; 1108.86 (2M + 23) + 34 4-f-ph H H Me n-bu 1H-NMR (DMSO-d ₆ ) δ 0.82-0.89 (m, 3H), 1.20-1.31 (m, 8H), 1.48-1.53 (m, 2H), 3.77-3.90 (m, 2H), 3.954.10 ( m, 3H), 4.214.45 (m, 2H), 556-5.61 (t, 1H), 5.83-6.20 (m, 3H), 7.18-7.25 (m, 4H), 7.55-758 (d, 1H), 11.50 (s. 1H); MC, m / e 584.1 (M + 23) + 35 3,4-diCl-Ph H H Me Et 1H-NMR (DMSO-d ₆ ) δ 1.12-1.31 (m, 9H), 3.77-3.92 (m, 2H), 3.954.08 (m, 3H), 4.214.45 (m, 2H), 5.56-5.62 ( t, 1H), 5.80-6.11 (m, 2H), 6.18-6.33 (m, 1H), 7.18-7.25 (m, 1H), 7.49-7.56 (d, 2H), 7.62-7.67 (m, 1H), 11.50 (s. 1H); MC, m / e 606.1 (M + 23) + 36 2-Cl-Ph H H Me i-pr 1H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.12-1.16 (m, 6H), 1.21-1.27 (m, 6H), 3.79-3.85 (m, 2H), 4.004.07 (m, 1H) , 4.284.32 (m, 1H), 4.38-4.43 (m, 1H), 4.834.87 (m, 1H), 5.56 (dd, J1 = 16.0 Hz, J = 8.0 Hz, 1H), 5.85-6.12 (m , 2H), 6.20-6.33 (m, 1H), 7.19-7.22 (m, 1H), 7.33 (t, J = 16.0 Hz, 1H), 7.48-755 (m, 3H), 11.55 (s, 1H) 37 4-MeO- H H Me Bn 1H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.19-1.26 (m, 6H), 3.69-3.70 (s,

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS Ph 3H), 3.87 (m, 2H), 3.99 (m, 1H), 4.20-4.21 (m, 1H), 4.35 (m, 1H), 5.07-5.09 (m, 2H), 554 (t, J = 16.0 Hz . 1H), 5.85-5.92 (m, 1H), 6.04-6.10 (m, 2H), 6.86 (d, J = 8.0 Hz. 2H). 7.09 (dd, J1 = 16.0 Hz, J2 = 4.0 Hz, 2H). 7.30-7.34 (m, 5H). 7.53 (s, 1H), 11.52 (s. 1H) 38 Ph H H Me n-pen 1H-NMR (DMSO-d ₆ ) δ 0.79-0.81 (m, 3H), 1.17-1.23 (m, 10H), 3.74-3.81 (m. 2H), 3.94-3.96 (m, 3H), 4.19-4.36 ( m, 2H), 5.49-5.54 (m, 1H), 5.87-6.08 (m, 3H), 7.14-7.33 (m, 3H), 7.31-7.35 (m, 2H), 7.51 (d, J = 8 Hz. 1H), 11.51 (s. 1H); MS, m / e 557.9 (M + 1) +; 1136.88 (2M + 23) + 39 4-cl-ph H H Me i-pr 1H-NMR (DMSO-d ₆ ) δ 1.04-1.19 (m, 12H), 3.76-3.80 (m, 2H), 3.98-4.08 (m, 1H), 4.42-4.42 (m, 2H), 4.82-4.85 ( m, 1H), 5.55-5.60 (m, 1H), 5.80-6.20 (m, 3H), 7.20-7.2 5 (m, 2H), 7.43 (d, J = 8.8 Hz, 1H), 7.54 (d, J = 8 Hz, 1H); 1151 (s, 1H); MS, m / e 563.88 (M + 1) +; 1148.73 (2M + 23) + 40 4-cl-ph H H Me n-bu 1H-NMR (DMSO-d ₆ ) δ 0.85 (t, J = 7.2 Hz, 3H), 1.22-1.33 (m, 8H), 1.45-1.53 (m, 2H), 3.80-3.87 (m, 2H), 3.96 -4.04 (m, 3H), 4.24-4.27 (m, 1H), 4.35-4.39 (m, 1H), 5.56-5.61 (m, 1H), 5.82-6.11 (m, 2H), 6.15-6.18 (m, 1H), 7.20-756 (m, 4H), 7.51-757 (m. 1H), 1154 (s. 1H); MC, m / e 577.95 (M + 1) + 41 4-cl-ph H H Me Et 1H-NMR (DMSO-d ₆ ) δ 1.14 (t, J = 7.0 Hz, 3H), 1.20-1.28 (m, 6H), 3.77-3.88 (m, 2H), 3.99-4.07 (m, 3H), 4.24 -4.28 (m, 1H), 4.34-4.43 (m, 1H), 5.56-5.61 (m, 1H), 5.86-6.13 (m, 2H), 6.15-6.24 (m, 1H), 7.20-7.26 (m, 2H), 7.44 (d, J = 7.6 Hz, 2H), 7.55 (d, J = 7.6 Hz, 1H), 1155 (s, 1H); MC, m / e 549.11 (M + 1) + 42 4-Me-Ph H H Me n-bu 1H-NMR (DMSO-d ₆ ) δ 0.79-0.83 (m, 3H), 1.17-1.28 (m, 8H), 1.45-1.47 (m, 2H), 2.22 (d, J = 2.8 Hz, 1H). 3.70-3.90 (m, 2H), 3.95-3.98 (m, 3H), 4.10-4.40 (m, 2H), 551 (t, 1H), 5.80-5.90 (m, 1H), 5.95-6.05 (m, 2H) ), 7.02-7.06 (m, 2H), 7.51 (t, J = 4.2 Hz. 4H), 7.51 (d, 1H), 11.51 (s, 1H); MS, m / e 557.99 (M + 1) +; 1136.84 (2M + 23) + 43 4-me-phe H H Me Bn 1H-NMR (DMSO-d ₆ ) δ 1.16-1.24 (m, 6H), 2.22 (s, 3H), 3.65-4.03 (m, 3H), 4.11-4.38 (m, 2H), 5.04-5.05 (m, 2H), 5.48-5.50 (m, 1H), 5.77-5.87 (m, 1H), 5.90-6.11 (m, 2H), 6.98-7.10 (m, 4H), 7.28-7.32 (m, 5H), 7.50 ( t, 1H), 11.48 (s, 1H); MC, m / e 592.00 (M + 1) +. 44 Ph H H Et Me 1H-NMR (DMSO-d ₆ ) δ 0.70-0.80 (m, 3H), 1.11-1.26 (m, 3H), 1.42-1.61 (m, 2H), 3.50-3.54 (m, 3H), 3.58-3.80 ( m, 2H), 3.91-4.02 (m, 1H), 4.12-4.38 (m, 2H), 5.47-5.52 (m, 1H), 5.90-6.03 (m, 2H), 7.08-7.16 (m, 3H), 7.26-7.35 (m, 2H), 7.48 (t, 1H), 11.45 (s, 1H); MS, m / e 515.95 (M + 1) +; 1052.82 (2M + 23) + 45 Ph H H Me 4-F-Bn ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ 1.20-1.26 (m, 6H), 3.80-3.93 (m, 2H), 3.98 (s, 1H), 4.25-4.26 (m, 1H), 4.36 -4.37 (m, 1H), 5.07 (s, 2H), 552-5.55 (m, 1H), 5.86-5.87 (m, 1H), 5.98-6.04 (m, 1H), 6.14-6.17 (m, 1H) , 7.15-7.20 (m, 5H), 7.36 (dd, J = 20.0.8.0 Hz, 4H), 7.54 (s, 1H), 1155 (s, 1H) 46 4-cl-ph H H Me n-bu ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ 1.21-1.28 (m, 6H), 3.71-3.88 (m, 1H), 3.91-3.98 (m, 1H), 4.00-4.01 (m, 1H) , 4.23-4.27 (m, 1H), 4.35-4.38 (m, 1H), 5.08 (d, J = 4.0 Hz, 2H), 5.57 (dd, J = 12.0, 8.0 Hz, 1H), 5.91 (d, J = 8.0 Hz, 1H), 6.01 (d, J = 8.0 Hz, 1H), 6.22-6.24 (m, 1H),

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 7.17-7.23 (m, 2H), 7.31-7.40 (m, 7H), 7.53 (s, 1H), 11.50 (s, 1H) 47 Ph H H Me 3-Me-1-Bu ¹ H-NMR (DMSO-d ₆ ) δ 0.80-0.82 (m, 6H), 1.18-1.40 (m, 8H), 1.50-1.58 (m, 1H), 3.71-3.82 (m, 3H), 3.97-3.4 .01 (m, 3H), 4.21-4.40 (m, 2H), 5.30 (t, J = 8.6 Hz, 1H), 5.81-6.10 (m, 3H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 7.48 (d, J = 8.4 Hz, 1H), 11.38 (s, 1H); MS, m / e 557.98 (M + 1) ⁺ ; 1136.88 (2M + 23) ⁺ 48 3,4-diCl-Ph H H Me Bn ¹ H-NMR (DMSO-d ₆ ) δ 1.05-1.37 (m, 6H), 3.71-3.82 (m, 1H), 3.87-4.02 (m, 2H), 4.28-4.29 (m, 1H), 4.36-4.38 (m, 1H), 5.04 (d, J = 5.2 Hz, 2H), 5.55-5.64 (m, 1H), 5.85-5.94 (m, 1H), 6.00-6.05 (m, 1H), 6.29-6.40 (m , 1H), 7.17-7.24 (m, 1H), 7.30-7.41 (m, 5H), 7.45-7.58 (m, 2H), 7.61 (d, J = 4.0 Hz, 1H), 11.53 (s, 1H); MS, m / e 545.80 (M + 1) ⁺ ; 49 Ph H H Me c-hex ¹ H-NMR (DMSO-d ₆ ) δ 1.18-1.41 (m, 12H), 1.59-1.67 (m, 4H), 3.74-13.80 (m, 1H), 3.96-4.02 (m, 1H), 4.19-4.26 (m, 1H), 4.31-4.39 (m, 1H), 4.60 (s, 1H), 552 (t, J = 7.8 Hz, 1H), 5.80-6.09 (m, 3H), 7.15-7.20 (m, 3H ), 7.32-7.36 (m, 2H), 7.52 (d, J = 8 Hz, 1H), 11.50 (s, 1H); MS, m / e 569.98 (M + 1) ⁺ ; 592.14 (M + 23) ⁺ fifty Ph H Me H n-bu ¹ H-NMR (DMSO-d ₆ ) δ 0.76 (t, J = 7.2 Hz, 3H), 1.10-1.22 (m, 8H), 1.38-1.43 (m, 2H), 3.72-3.75 (m, 2H), 3.87-3.93 (m, 3H), 4.14-4.21 (m, 1H), 4.23-4.33 (m, 1H), 5.46-5.54 (m, 1H), 5.84-6.11 (m, 3H), 7.09-7.14 (m , 2H), 7.27-7.32 (m, 2H), 7.34-751 (m, 1H), 11.47 (s. 1H); MC, m / e 543.98 (M + 1) ⁺ 51 Ph H Me H i-pr ¹ H-NMR (DMSO-d ₆ ) δ 1.39 (d, J = 7.2 Hz, 6H), 1.19-1.29 (m, 6H), 3.65-3.75 (m, 2H), 3.95-4.05 (m, 1H), 4.20-4.22 (m, 1H), 4.31-4.33 (m, 1H), 4.79-4.82 (m, 1H), 5.48-5.57 (m, 1H), 5.84-5.91 (m, 1H), 5.96-6.07 (m , 2H), 7.12-7.35 (m, 5H), 7.44-754 (m. 1H), 11.49 (s, 1H); MC, m / e 529.96 (M + 1) ⁺ 52 Ph H Me H Bn ¹ H-NMR (DMSO-d ₆ ) δ 1.18-1.28 (m, 6H), 3.70-3.83 (m, 1H), 3.87-3.94 (m, 1H), 3.99-4.01 (m, 1H), 4.23-4.26 (m, 1H), 4.33-4.37 (m, 1H), 5.03-5.12 (m, 2H), 5.51-559 (m, 1H), 5.87-5.90 (m, 1H), 5.95-6.07, (m, 1H ), 6.10-6.27 (m, 1H), 7.15-7.23 (m, 3H), 7.31-7.38 (m, 7H), 7.47-756 (m, 1H), 1150 (s, 1H); MC, m / e 577.99 (M + 1) ⁺ 53 2-Cl-Ph H H Me n-bu ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ 0.81-0.86 (m, 3H), 1.21-1.31 (m, 8H), 1.46-1.52 (m, 2H), 3.84-3.90 (m, 2H) , 3.97-4.04 (m, 3H), 4.27-4.41 (m, 2H), 553-558 (m, 1H), 5.82-5.95 (m, 1H), 5.96-6.10 (m, 1H), 6.27-6.31 ( m, 1H), 7.19-7.22 (m, 1H), 7.34 (dd, J = 8.0.4.0 Hz, 1H), 7.47-755 (m, 3H), 1155 (s, 1H) 54 4-br-ph H H Me i-pr ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ 1.10-1.14 (m, 6H), 1.20-1.27 (m, 6H), 3.74-3.81 (m, 2H), 3.99-4.01 (m, 1H) , 4.21-4.25 (m, 1H), 4.37-4.38 (m, 1H), 4.81-4.85 (m, 1H), 5.58 (dd, J = 8.0.4.0 Hz, 1H), 5.82-5.95 (m, 1H) , 5.96-6.09 (m, 1H), 6.10-6.13 (m, 1H), 7.18 (dd, J = 12.0. 8.0 Hz, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) 55 4-f-ph H H Me c-hex ¹ H-NMR (DMSO-d ₆ ) δ 1.20-1.44 (m, 12H), 1.60-1.71 (m, 4H), 3.75-4.02 (m, 2H), 3.94-4.02 (m, 1H), 4.19-4.26 (m, 2H), 4.59-4.61 (m, 1H), 557 (t, J = 8.4 Hz, 1H), 5.85-6.06 (m, 3H), 7.17-7.23 (m, 4H), 7.54 (d, J = 8.4 Hz, 1H); 11.50 (s, 1H); MC, m / e 587.92 (M + 1) ⁺ 56 4-br-ph H H Me c-hex ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ = 1.18-1.46 (m, 12H), 1.61-1.69 (m,

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 4H), 3.75-3.82 (m, 2H), 3.95-4.08 (m, 1H), 4.25-4.28 (m, 1H), 4.38 (s, 1H), 4.60-4.62 (m, 1H), 5.56-5.60 ( m, 1H), 5.82-5.95 (m, 1H), 6.02-6.20 (m, 2H), 7.09-7.20 (m, 2H), 7.53-7.57 (m, 3H), 11.52 (s, 1H) MC, m / e 650.0 (M + 3) ⁺ 57 Ph H H Et i-pr ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ = 0.75-0.82 (m, 3H), 1.12-1.26 (m, 9H), 1.52-1.59 (m. 2H), 3.55-3.68 (m, 1H ), 3.72-3.85 (m, 1H), 3.95-4.08 (m, 1H), 4.18-4.28 (m, 1H), 4.32-4.41 (m, 1H), 4.83-4.86 (m, 1H), 555 (m , J = 7.6 Hz, 1H), 5.99-6.04 (m, 2H), 6.05-6.10 (m, 1H), 7.14-7.21 (m, 3H), 7.33-7.37 (m, 2H), 752-754 (m , 1H); 1153 (s, 1H); MC, m / e 566.07 (M + 23) ⁺ 58 Ph H H Et c-hex ¹ H-NMR (400 MHz, DMSO-d ₆ ): δ 0.75-0.88 (m, 3H), 1.26-1.46 (m, 9H), 1.52-1.69 (m, 6H), 3.60-3.63 (m, 1H) , 3.72-3.90 (m, 1H), 4.02-4.03 (m, 1H), 4.24-4.27 (m, 1H), 4.37-4.38 (m, 1H), 4.63-4.65 (m, 1H), 5.55 (dd, J = 8.0 G C, 4.4 Hz, 1H), 5.80-5.95 (m, 1H), 6.00-6.07 (m, 2H), 7.15-7.22 (m, 3H), 7.34-7.38 (m, 2H), 754 ( d, J = 8.0 Hz, 1H), 1155 (s, 1H); MS, m / e 584.01 (M + 1) ⁺ , 606.17 (M + 23) ⁺ 59 4-f-ph H H Et c-hex ¹ H-NMR (DMSO-d ₆ ) δ 0.75-0.84 (m, 3H), 1.24 (d, J = 22.8 Hz, 3H), 1.29-1.47 (m, 6H), 151-1.70 (m, 6H), 3.59-3.66 (m. 1H), 3.77-3.84 g, (m, 1H), 3.98-4.04 (m, 1H), 4.21-4.27 (m, 1H), 4.34-4.41 (m, 1H), 4.60-4.65 (m, 1H), 5.56-5.60 (m, 1H), 5.84-5.90 (m, 1H), 6.00-6.08 (m, 2H), 7.20-7.24 (m, 4H), 756 (d, J = 8.0 Hz , 1H); 11.49 (s, 1H); MS, m / e 602.00 (M + 1) ⁺ 60 Ph H H Me F-CH ₂ -CH ₂ - ¹ H-NMR (DMSO-d ₆ ) δ 1.18-1.25 (m, 6H), 3.71-3.89 (m, 2H), 3.92-3.99 (m, 1H), 4.19-4.27 (m, 4H), 4.48-4.61 (m, 2H), 3.94-3.98 (m. 2H), 4.1-4.23 (m, 4H), 5.47-5.52 (m, 1H), 6.01-6.11 (m, 1H), 5.90-6.14, (m, 2H) ), 7.15-7.21 (m, 3H), 7.32-7.36 (m, 2H), 7.46-7.57 (m, 1H), 11.49 (s, 1H); MC, m / e 533.86 (M + 1) ⁺ 61 Ph H H Me F ₂ CH-CH ₂ - ¹ H-NMR (DMSO-d ₆ ) δ 1.17-1.24 (m, 6H), 3.67-3.81 (m, 1H), 3.89-3.98 (m, 2H), 4.21-4.36 (m, 4H), 5.48-553 (m, 1H), 5.82-6.05 (m, 2H), 6.18-6.22 (m, 2H), 7.15-7.20 (m, 3H), 7.32-7.36 (m, 2H), 751 (s, 1H), 1150 (s, 1H); MS, m / e 551.92 (M + 1) ⁺ ; 62 Ph H H Me (CF ₃ ) ₂ -CH- ¹ H-NMR (DMSO-d ₆ ) δ 1.13-1.29 (m, 6H), 3.67-3.81 (m, 1H), 3.94-4.32 (m, 4H), 5.47 (t, J = 8 Hz 1H), 5.82 -6.01 (m, 2H), 6.33-6.36 (m, 1H), 6.70-6.78 (m, 1H), 7.09-7.15 (m, 3H), 7.28-7.32 (m, 2H), 7.43-7.46 (m, 1H), 11.44 (s, 1H); MS, m / e 637.90 (M + 1) ⁺ 63 Ph H H Me (CH ₂ F) ₂ -CH- ¹ H-NMR (DMSO-d ₆ ) δ 1.20-1.29 (m, 6H), 3.70-3.90 (m, 1H), 3.91-4.12 (m, 2H), 4.20-4.33 (m, 1H), 4.35-4.48 (m, 1Н), 4.52-4.55 (m, 2Н), 4.63-4.67 (m, 2Н), 5.20-5.35 (m, 1Н), 5.56 (t, J = 8.4 Hz, 1Н), 5.80-5.95 (m , 1H), 5.95-6.10 (m, 1H), 6.18-6.21 (m, 1H), 7.18-7.23 (m, 3H), 7.35-7.39 (m, 2H), 7.54 (s, 1H), 11.55 (s , 1H); MS, m / e 565.98 (M + 1) ⁺

Etc. R ¹ R ² R ^3a R ^3b R ⁴ NMR / MS 64 Ph H H Me c-Pr-CH ₂ - ¹ H-NMR (DMSO-d ₆ ) δ 0.20-0.24 (m, 2H), 0.47-0.48 (m, 2H), 0.76-0.84 (m, 3H), 1.03-1.05 (m, 1H), 1.23 (dd , J = 22.4 6.8 Hz 3H), 1.55-1.60 (m, 2H), 3.61-3.68 (m, 1H), 3. 81-3.89 (m, 3H), 3.984.03 (m, 1H), 4.234.29 (m, 1H), 4.354.41 (m, 1H), 5.56-6.00 (m, 1H), 5.88-5.91 (m, 1H), 6.04-6.10 (m, 2H), 7.20-7.24 (m, 4H) . 7.55 (d, J = 7.6 Hz 1H); 11.53 (s, 1H); MC, m / e 573.17 (M + 1) ⁺ 65 Ph H H Et c-pen ¹ H-NMR (DMSO-d ₆ ) δ 0.75-0.83 (m, 3H), 1.20-1.28 (m, 3H), 1.49-1.63 (m, 8H), 1.76-1.80 (m, 2H), 3.58-3.60 (m, 1H), 3.70-3.82 (m, 1H), 3.984.05 (m, 1H), 4.24-4.26 (m, 1H), 4.374.42 (m, 1H), 5.03 (s, 1H), 5.54 -5.57 (m, 1H), 5.90-6.00 (m, 1H), 6.02-6.07 (m, 2H), 7.15-7.22 (m, 3H), 7.35-7.39 (m, 2H) 7.55 (d, J = 8 , 0 G q, 1H); 11.55 (s, 1H); MC, m / e 570.03 (M + 1) ⁺ * R ² and R ^3b together represent - (CH ₂ ) ₃ - as a derivative of L-proline

Purification process prep-HPLC (high performance liquid chromatography)

The crude products were dissolved in methanol. The volumes of injected samples of these solutions were 5 ml.

The preparative HPLC system includes 2 Gilson 306 pumps, a Gilson 156 UV / Vis detector, a Gilson 215 fraction injector and collector, with Unipoint control software. A Ymc 25 × 30 × 2 mm column was used. The mobile phase was water qualified for HPLC (A) and qualified for HPLC acetonitrile (B). Fractions were placed in 100 * 15 mm glass tubes.

The HPLC gradient is shown in Table 1. When the gradient was selected, the acetonitrile solution was added to the HPLC system, and then the fractions were collected according to UV peaks. After separation, each glass tube passed an MS test to select the desired compounds. Fractions with the desired MS were collected in a carefully weighed flask. Most of the acetonitrile was removed under reduced pressure, and the remaining solution was lyophilized to obtain the desired compound.

Table 1: Preparative HPLC gradient Time (min) Flow rate (ml / min) % BUT %AT 0 fifteen 90 10 thirty fifteen 60 40

Received Example 66

Preparation of Compound (b)

To a solution of compound a (1 g 2.69 mmol) in anhydrous THF (30 ml) was added dropwise to a 1M solution of LiAl (OBu-t) ₃ H in THF (2.69 ml, 2.69 mmol) at -20 ° C.

The reaction mixture was stirred for 2-3 hours at the same temperature. EtOAc (100 ml) was added, then a saturated solution of NH ₄ Cl (10 ml) was added, and the reaction mixture was gradually brought to room temperature. The reaction mixture was extracted with EtOAc and washed with IN HCl and water. The combined organic phase was evaporated to give 0.8 g of crude compound b in the form of a colorless oil, which was directly used in the next reaction.

Preparation of Compound (d)

To a solution of compound b (0.8 g, 2.1 mmol), compound c (0.45 g, 2.5 mmol) and Ph ₃ P (0.56 g, 2.1 mmol) in anhydrous THF (20 ml) in a nitrogen atmosphere, DEAD (1.8 ml) was added. The reaction mixture was stirred overnight at room temperature. The reaction solution was concentrated under reduced pressure. The precipitate was separated by preparative layer chromatography (hexanes: EtOAc = 3: 1) to obtain crude compound d (0.8 g). The crude compound d was used in the next step without further purification.

Preparation of Compound (e)

Compound d (0.8 g, 1.57 mmol) was diluted in THF (2 ml), and then ammonium saturated THF (5 ml) was added to this solution. The reaction mixture was heated at 90 ° C. overnight. After 18 hours, the solution was cooled with ice water to room temperature, then the solvent was removed under reduced pressure, and the residue was purified on a column to obtain compound e (0.75 g) for the next step.

Preparation of Compound (f)

Compound e (0.5 g, 1.01 mmol) was dissolved in methanol (2 ml), and methanol saturated with ammonium (5 ml) was added to the solution. The reaction mixture was stirred at room temperature overnight. After 18 hours, the solution was cooled with ice water to room temperature, then the solvent was removed under reduced pressure, and the precipitate was purified on a column to obtain crude compound f (0.15 g) for the next step.

Obtaining compound (i)

A solution of triethylamine (1.07 g, 10.6 mmol) in anhydrous dichloromethane (15 ml) was added dropwise to a solution of compound g (1.16 g, 5.3 mmol) and compound h (1.31 g, 5.3 mmol) in dichloromethane (10 ml) with vigorous stirring at -78 ° C for 2 hours. After the addition was complete, the reaction temperature was allowed to gradually drop to room temperature and was stirred overnight. Then, the solvent was removed in vacuo and anhydrous ether (20 ml) was added, the precipitated salt was filtered, and the precipitate was washed with ether. The combined organic phase was concentrated to obtain a colorless oil, which is compound i (1.0 g).

Getting connection 66

To a solution of compound j (0.1 g, 0.35 mmol) which was diluted in 10 ml of anhydrous THF was stirred, and to which 0.4 g of NMI was added until the solution became clear, compound i (0.8 g, 2.89 mmol) was added in 10 ml of THF dropwise, and stirred at room temperature. temperature during the night. The purity and identification of the compound was confirmed by LCMS. The solvent was evaporated and purified by prep-HPLC to give 66. (25 mg, Yield: 13.6%). ¹ H NMR (DMSO-4) 8 1.08 (d, J = 22.8 Hz, 3H), 1.17-1.24 (m, 3H), 3.50-3.52 (m, 3H), 3.78-3.83 (m, 1H), 4.10- 4.13 (m, 1H), 4.24-4.44 (m, 2H), 5.85-5.92 (m, 1H), 6.01-6.11 (m, 1H), 6.2.-6.27 (m, 1H), 7.08-7.19 (m, 4H), 7.31-7.38 (m, 3H), 8.15 (s, 1H), 8.26 (s, 1H); MS, m / e 525 (M + 1) ⁺ .

Examples 67-74, disclosed below, were prepared using the same processes as described above for Example 66.

Example R ¹¹ R ¹⁰ NMR / MS 67 OH NH ₂ ¹ H NMR (DМSO-d ₆ ) δ 1.06-1.13 (m, 3H), 1.20-1.24 (m, 3H), 3.27-3.33 (m, 3H), 3.56 (s, 1H), 3.82-3.88 (m, 1H), 4.07-4.13 (m, 1H), 4.25-4.40 (m, 2H), 5.85-5.87 (m, 1H), 5.98-6.09 (m,

Example R ¹¹ R ¹⁰ NMR / MS 2H), 6.59 (s, 32H), 7.14-7.37 (m, 3H), 7.35-7.37 (m, 2H), 7.79 (d, 7 = 7.2 Hz, 1H), 10.69 (s, 1H); MS, m / e 541 (M + 1) ⁺ ; 68 NH ₂ NH ₂ ¹ Н NMR (DМSO-d ₆ ) δ 1.07 (d, 7 = 22.8 Hz, 3Н), 1.19 (d, 7 = 7.2 Hz, 3Н), 3.51 (s, 3Н), 3.62 (s, 1Н), 3.75- 3.81 (m, 1H), 4.05-4.11 (m, 1H), 4.27-4.42 (m, 2H), 5.79-5.83 (m, 1H), 5.92 (s, 2H), 6.00-6.09 (m, 2H), 6.75 (s, 2H), 7.08-7.17 (m, 3H), 7.31-7.35 (m, 2H), 7.78 (s, 1H); MS, m / e 540 (M + 1) ⁺ ; 69 NH ₂ c-pentyl1-NH- ¹ Н NMR (DМSO-d ₆ ) δ 1.05 (d, 7 = 22.8 Hz, 3Н), 1.09-1.19 (m, 3Н), 1.48 (s, 4Н), 1.66 (s, 1Н), 1.86 (s, 1Н ), 3.54 (d, 7 = 14 Hz, 3H), 3.65 (s, 1H), 4.25-4.43 (m, 4H), 5.71-5.82 (m, 1H), 5.94-6.04 (m, 4H), 7.11- 7.24 (m, 3H), 7.26-7.34 (m, 2H), 7.77 (d, 7 = 3.6 Hz, 1H); MS, m / e 608 (M + 1) ⁺ 70 NH ₂

¹ N NMR (DМSO-d ₆ ) δ 1.07 (d, 7 = 22.4 Hz, 3Н), 2.35-2.38 (m, 2Н), 3.54 (d, 7 = 9.2 Hz, 3Н), 3.59-3.62 (m, 2Н ), 3.65 (s, 1H), 3.75-3.82 (m, 1H), 4.01-4.13 (m, 2H), 4.22-4.40 (m, 6H), 5.75-5.85 (m, 1H), 6.00-6.07 (m , 4H), 7.15-7.21 (m, 3H), 7.32-7.35 (m, 2H), 7.79 (d, J = 4.0 Hz, 1H); MC, m / e 580 (M + 1) + 71 NH ₂ Et ₂ N- ¹ H NMR (DMSO-d ₆ ) δ 1.06-1.28 (m, 12H), 3.55 (d, J = 4.8 Hz, 3H), 3.79-3.87 (m, 4H), 4.07-4.12 (m, 2H), 4.29 -4.42 (m, 3H), 5.75-5.82 (m, 1H), 5.94 (s, 2H), 6.04-6.10 (m, 2H), 7.14-7.22 (m, 3H), 7.31-7.37 (m, 2H) 7.82 (d, J = 4.4 Hz, 1H); MC, m / e 596 (M + 1) ⁺ 72 NH ₂ N-propyl 1-NH- ¹ Н NMR (DМSO-d ₆ ) δ 0.84 (t, J = 7.2 Hz, 3Н), 1.01-1.01 (m, 3Н), 1.09-1.12 (m, 3Н), 1.51-1.56 (m, 2H), 3.48 (d, / = 15.2 Hz, 3H), 3.79-3.82 (m, 1H), 4.04-4.05 (m, 1H), 4.27-4.38 (m, 3H), 5.72-5.79 (m, 1H), 5.98-6.04 (m, 4H), 7.13-7.20 (m, 3H), 7.26-7.32 (m, 2H), 7.76 (d, J = 5.2 Hz, 1H); MC, m / e 582 (M + 1) ⁺ 73 NH ₂ c-butyl-NH- ¹ H NMR (DMSO-d ₆ ) δ 1.02-1.08 (m, 3H), 1.18 (d, J = 4.8 Hz, 3H), 1.44-1.61 (m, 2H), 2.02-2.17 (m, 4H), 3.51 (d, J = 10.8 Hz, 3H), 3.78-3.83 (m, 1H), 4.03-4.06 (m, 1H), 4.27-4.38 (m, 2H), 4.53-4.62 (m, 1H), 5.68-5.79 (m, 1H), 5.95-6.04 (m, 4H), 7.11-7.18 (m, 3H), 7.29-7.35 (m, 2H), 7.51-7.58 (m,

Example R ¹¹ R ¹⁰ NMR / MS 1H), 7.78 (d, J = 5.2 Hz, 1H); MC, m / e 594 (M + 1) ⁺ 74 NH ₂

¹ H NMR (DMSO-d ₆ ) δ 0.97-1.20 (m, 6H), 2.18 (s, 3H), 2.19 (s, 4H), 3.43-3.47 (m, 3H), 3.75 (s, 1H), 4.01 -4.06 (m, 4 H), 4.22-4.35 (m, 3H), 5.69-5.75 (m, 1H), 5.98-6.05 (m, 3H), 7.09-7.15 (m, 3H), 7.25-7.29 (m , 2H), 7.77 (d, J = 3.6 Hz, 1H); MC, m / e 623 (M + 1) ⁺

Examples numbered 75-80 are prepared using the same processes as described above for example 66.

Example R ¹¹ R ¹⁰ 75 N n-propyl-NH- 76 N c-butyl NH- 77 n c-pentyl-NH- 78 n

79 n

80 n

EXAMPLE 81

Some of the exemplified compounds were prepared as a mixture of diastereomers due to the chirality of the phosphorus atom. The diastereomers were separated on a Chiralpak-AS-H (2 × 25 cm) column under ultra-high temperature liquid chromatography (SFC) conditions using 20% methanol in carbon dioxide as a solvent. The absolute stereochemistry of the P-chiral center of diastereomers has not been determined. However, the resolution of these two diastereomers gives an idea of isomers characterized as rapidly eluting and slowly eluting. Some examples are given below.

Compound EC90 (uM) Example 15 (Mixture of diastereomers) 0.86 The fast moving isomer of Example 15 1.35 Slow moving isomer from Example 15 0.26 Example 39 (Mixture of diastereomers) 0.47 The fast moving isomer of Example 39 0.78 Slow Moving Isomer from Example 39 0.02 Example 49 (Mixture of diastereomers) 0.126 The fast moving isomer of Example 49 0.03 Slow moving isomer from Example 49 5.78

EXAMPLE 82

HCV replicon assay. HCV RNA-containing Huh7 RNA cells (clone A cells; Apath, LLC, St. Louis, Mo.) were maintained exponentially in Dulbecco's modified Eagle's medium (high glucose) containing 10% fetal bovine serum, 4 mM L -glutamine and 1 mM sodium pyruvate, 1 x non-essential amino acids, and G418 (1,000 Ig / ml). Antivirus analysis was performed on the same medium without G418. Cells were seeded on a 96-well plate, 1,500 cells per well, and test compounds were added directly immediately after plating. The incubation time was 4 days. At the end of the incubation step, total cellular RNA (RNeasy 96 kit; Qiagen) was isolated. Replicon RNA and internal control (TaqMan control reagents for tRNA; Applied Biosystems) were amplified in a single-step multi-channel RT-PCR protocol, as recommended by the manufacturer. HCV primers were designed using Primer Express software (Applied Biosystems) and closed with highly conservative 5'-untranslated (UTR) sequences (sense, 5'-AGCC ATGGCGTTAGTA (T) G AGTGT-3 ', and antisense, 5'- TTCCGCAGACCACTATGG-3 '; test, 5'-FAM-CCTCCAGGACCCCCCCCCTCCC-TAMRA-3').

To express antiviral efficacy, the threshold of the RT-PCR cycle of the test compound was subtracted from the average threshold of the RT-PCR cycle of the control without the drug (ΔCt _hcv ) -ΔCt of 3.3 equals a 10-fold decrease in 1-log (equals 90% effective concentration [ec90]) in replicon levels RNA The cytotoxicity of the test compound can also be expressed in terms of ΔCt _rna . Then, the specificity parameter ΔΔCt can be represented as (ΔCt _hcv -ΔСt _rrnc ), where HCV RNA levels are normalized for rRNA levels and calibrated against the control without the drug.

Etc # Compound Log10 50 μM Reduction EC90 (μM) 5

-1.21 3.0 6

-0.45 Nd 7

0.31 Nd

Etc # Compound Log10 50 μM Reduction EC90 (μM) 8

-1.48 2.11 10

-1.25 19.15 eleven

-0.55 Nd 12

0.31 Nd fifteen

Nd 0.86 25

-2.22 0.39 27

-2.25 0.66

Etc # Compound Log10 50 μM Reduction EC90 (μM) 28

-2.16 0.75 36

-1.64 21.9 39

-1.78 0.47 49

-2.69 0.126 53

-1.33 <0.3 54

-1.55 0.57

Etc# Compound Log10 50 μM Reduction EC90 (μM) 55

-2.38 <0.3 69

-2.25 <0.3 70

-2.25 <0.3 ¹ (4-BrPh): 4-bromophenyl.

Claims (14)

1. Isopropyl ether (S) -2 - {[(2R, 3R, 4R, 5R) -5- (2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-yl) -4-fluoro- 3-hydroxy-4-methyl-tetrahydrofuran-2-ylmethoxy] -phenoxy-phosphorylamino} -propionic acid or its stereoisomer. 2. An antiviral composition comprising a compound according to claim 1 and a pharmaceutically acceptable medium. 3. A composition for treating hepatitis C virus, containing an effective amount of a compound according to claim 1 and a pharmaceutically acceptable medium. 4. A method of treating a subject infected with a virus, comprising administering to the subject an effective amount of a compound according to claim 1, wherein the virus is selected from hepatitis C virus, West Nile fever virus, yellow fever virus, dengue virus, rhinovirus, poliovirus, hepatitis A virus, diarrhea virus cattle, and Japanese encephalitis virus. 5. A method of treating hepatitis C virus infection in a subject in need of such treatment, comprising: the introduction to the specified subject an effective amount of a compound according to claim 1. 6. The method of obtaining the compound or its stereoisomer according to claim 1, including: the interaction of compound 4 "with the nucleoside analogue 5 '

, where X 'represents a leaving group. 7. A product containing a compound according to claim 1, obtained by a method including: the interaction of compound 4 "with the nucleoside analogue 5 '

where X 'represents a leaving group.